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Pharmac full

Pharmacology

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72 views

Pharmac full

Pharmacology

Uploaded by

mdriyanj
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
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INDEX

SI. NO. TOPIC PAGE


01 Local anaesthesics 03
02 General anaesthetics 04
03 CNS Depressants – Sedatives & Hypnotics, Tranquilisers 05
04 NSAIDs, Antipyretics & Analgesics 06
05 Anti-epileptics 08
06 Anti-hypertensive 09
07 Anti-anginal, Anti-platelet 10
08 Hypolipidaemic, Haemopoetic, Coagulants 11
09 Bronchodialators, Aerosols/Inhalants 12
10 Expectorants 13
11 Digestants, Carminatives 14
12 Anti-ulcer 15
13 Laxatives 16
14 Anti-diarrhoeal 18
15 Anti-emetics 19
16 Hepato-protectives 20
17 Diuretics 21
18 Anti-diuretics 22
19 Hormonal therapy 23
20 Anti-obesity 24
21 Anti-diabetics 25
22 Anti-thyroid 26
23 Oxytocics, Galactagogues 27
24 Contraceptives 28
25 Anti-histamine 30
26 Anti-microbial 31
27 Anti-biotics 33
28 Anti-malarial 35
29 Amoebicidal, Antifilarial, Anthelmentic 37
30 Antifungal 38
31 Vitamins & Minerals 39
32 Water imbalance & IV fluids 41
33 Vaccins 43
34 Antivenom & Antirabbies 44
35 Local antiseptics 47
36 Drugs in ophthalmic practice 48
37 Anticancer drugs 50
38 Immuno moddulators 51

Alpesh B. Munjani
With the help of Dravyaguna department
J.S.Ayurveda Mahavidhyalaya, Nadiad.

1 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


2 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17
LOCAL ANAESTHETICS
LAs are drugs which upon topical application or local injection causes reversible loss of sensory perception, especially
of pain, in restricted area of the body.

LA blocks generation & conduction of nerve impulse at all parts of neuron where they come in contact, without
causing any structural damage. Thus, not only sensory but also motor impulses are interrupted when LA is applied to
mixed nerve, resulting in musclular paralysis & loss of autonomic control as well.

Classification:-

1. Injectable (i) Low potency & Short duration


 Procaine
 Chlroprocaine

(ii) Intermediate potency & duration


 Lidocaine (Lignocaine)
 Prilocaine

(iii) High potency & Long duration


 Tetracaine
 Bupivacaine
 Cinchocaine

2. Surface (i) Soluble


 Lidocaine (Lignocaine)
 Tetracaine
 Cocaine

(ii) Insoluble
 Benzocaine
 Oxethazaine

Mechanism of action :-

Concentration of LA increases

Rate of rise of AP & maximum depolarization decreases

Slowing of conduction

Fails to reach the thresold potential

Conducation block

3 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


GENERAL ANAESTHETICS

GAs are drugs which produce reversible loss of all sensation & conciousness.

The cardinal fetures of GA are;


 Loss of all sensations, especially pain
 Sleep & Amnesia
 Immobility & muscle relaxation
 Abolition of somatic & autonomic reflexs

Classification:-

1. Inhalational (i) Gas


 Nitrous oxide (N2O)

(ii) Volatile liquids


 Ether
 Isoflurane
 Desflurane
 Enflurane

2. Intravenous (i) Inducing agents


 Propofol
 Etomidate
 Thiopentone

(ii) Slower acting drugs


 Benzodiazepines
- Diazepam
- Lorazepam
- Midazolam

 Dissociative :- Catemine

 Opioid analgesia :- Fentanyl

Comparative features of general and local anaesthesia :-


LOCAL ANAESTHESIA GENERAL ANAESTHESIA
1. Site of action Peripheral nerves CNS
2. Area of body involved Restricted area Whole body
3. Consciousness Unaltered Lost
4. Care of vital functions Usually not needed Essential
5. Physiological trespass Low High
6. Poor health patient Safer Risky
7. Use in non-cooperative patient Not possible Possible
8. Major surgery Cannot be used Preferred
9. Minor surgery Preferred Not preferred

4 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


CNS DEPRESSANTS

1. Sedatives :- are the drugs which reduces excitement, calms the subject without producing sleep, though
drowsiness can be produced. Commonly used as Anxiolytics.

2. Hypnotics :- are th drugs which induce or maintain sleep similar to normal arousable sleep.

Sedatives & Hypnotics both are CNS depressants with somewhat differing time action & dose relationship.

Treatment of insomnia is the most important use of this class of drugs.

Classification:-

1. Barbiturates (i) Long acting


 Phenobarbitone

(ii) Short acting


 Butobarbitone
 Pentobarbitone

(iii) Ultra short acting


 Thiopentone

2. Benzodiazepines (i) Hypnotic


 Diazepam
 Flurazepam
 Alprazolam
 Triazolam

(ii) Anti-anxiety
 Diazepam
 Alprazolam
 Oxazepam
 Lorazepam

(iii) Anti-convulsant
 Zopiclone
 Zolpidem
 Zaleplon

3. Newer Non-Benzodiazepine Hypnotics  Zopiclone


 Zolpidem
 Zaleplon

Tranquilizer :- is an old term meanins ‘A drug which reduces mental tension & produces calmness without inducing
sleep or depressing mental faculties.’ E.g, benzodiazepines.

5 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


Non-Steroidal Anti-inflammatory Drugs & Antipyretics – Analgesics

ANTI-INFLAMMATORY :- are the agents usefull in treatment of inflammatory conditions.

ANTIPYRETICS :- are the drugs which reduce body temperature in fever but do not cause hypothermia in
normothermic individulas.

ANALGESICS :- are the drugs which relieve pain without causing loss of conciousness.

Classification:-

1. Non-selective COX inhibitors (i) Salicylates


(Traditional NSAIDs)  Aspirin

(COX = cylco-oxygenase) (ii) Propionic acid derivatives


 Ibuprofen
 Ketoprofen

(iii) Anthranilic acid derivative


 Mephenamic acid

(iv) Aryl-acetic acid derivatives


 Diclofenac
 Aceclofenac

(v) Oxicam derivatives


 Piroxicam
 Tenoxicam

(vi) Pyrrolo-pyrrole derivatives


 Ketorolac

(vii) Indole derivative


 Indomethacin

2. Preferential COX-2 inhibitors  Nimesulide


 Meloxicam
 Nabumetone
3. Selective COX-2 inhibitors  Celecoxib
 Etoricoxib
 Parecoxib

4. Analgesic-Antipyretics, (i) Para-amino-phenol derivative


with poor anti-inflammatory action  Paracetamol (Acetaminophen)

(ii) Pyrazolon derivatives


 Metamizol
 Propiphenazone

(iii) Benzoxazocine derivative


 Nefopam

6 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


Uses :-

(i) As analgesic for headache, backache, myaglia, joint pain, pulled muscle, toothache, dysmenorrhoea.
(ii) As antipyretic It is efffective in fever of any origin; dose same as analgesics. Anti-pyretics are not usefull in fever
due to heat stroke.
(iii) In Acute rheumatic fever
(iv) In Rheumatoid arthritis
(v) In Osteoartheritis

Mechanism of action :-

Antipyresis mechanism :- Fever during infection is produced through the generation of pyrogenes which induce
PGE2 (Prostaglandin E2, Also known as Dinoprostone ) production in hypothalamus – raise its temperature set point.
NSAIDs block the action of pyrogene & reduces body temperature.

Analgesia mechanism :- PGs induce hyperalgesia by affecting the transducing property of free nerve ending. NSAIDs
do not affect the tenderness induced by direct application of PGs, but block the pain sensitizing mechanism induced
by analgesic substances. So, they are more effective againts inflammation associated pain.

Side effects :-

 Nausea
 Vomiting
 Epigastric distress
 Increased occult blood loss in stool
 Gastric mucosal damage
 Peptic ulceration

7 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


ANTI-EPILEPTICTS

Antiepilepticts are the drugs usefull in treatment of epilepsy. Epilepsy is a collective term for a group of chronic
seizures having common sudden and transient episodes of disterbance of consiousness and/or a charecteristic body
movement and sometimes autonomic hyperactivity.

Classification:-

1. Barbiturate  Phenobarbitone

2. Deoxybarbiturate  Primidone

3. Hydantoin  Phenytoin
 Fosphenytoin

4. Iminostilbene  Carbamazepine
 Oxcarbazepine

5. Succinimide  Ethosuximide

6. Alophatic Carboxylic Acid  Valproic acid


 Divalprox

7. Benzodiazepines  Clonazepam
 Diazepam
 Lorazepam
 Clobazam

8. Phenyltriazine  Lamotrigine

9. Cyclic GABA analouge  Gabapentin

10. Newer Drugs  Vigabatrin


 Topiramate
 Tiagabine
 Zonisamide
 Levetiracetam

8 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


ANTI-HYPERTENSIVE

These drugs used to lower blood pressure in hypertension.

Classification:-

1. Diuretics (i) Thiazides


 Chlorothalidone
 Indapamide

(ii) High ceilling


 Flurasemide

(iii) K+ Sparing
 Spironolactone
 Amiloride

2. ACE inhibitors  Captopril


 Lisinopril
 Ramipril
 Enalapril

3. Angiotensin (AT1) receptor blockers  Losartan


 Irbesartan
 Valsartan
 Candesartan

4. Calcium channel blockers  Lacidipine


 Felodipine
 Amlodipine

5. β adrenergic blockers  Propranolol


 Metaprolol
 Atenolol

6. α adrenergic blockers  Terazosin


 Doxazosin

7. β + α adrenergic blockers  Labetalol


 Carvedilol

8. Central sympatholytic  Clonidine


 Methyldopa

9. Vasodilators (i) Arteriolar


 Minoxidil
 Diazoxide

(ii) Arteriolar + venous


 Sodium nitroprusside

9 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


ANTI-ANGINAL
Antianginal drugs are those that prervent, abort or terminate attacks of angina pectoris.

Angina pectoris ls a pain syndrome due to indurction of an adverse oxygen supply / demand situation in a portion of
the myocardium.

Classification:-

1. Nitrates (i) Short acting :-


 Glyceryl trinitrate (GTN)

(ii) Long acting :-


 Isosorbide dinitrate
 Erythrityl tetranitrate
 Pentaerythritol tetranitrate

2. β Blocker  Propranolol
 Metoprolol
 Atenolol

3. Calcium Channel Blockers (i) Phenyl alkylamine :-


 Verapamil

(ii) Benzothiazepine :-
 Diltiazem

(iii) Dihydropyridines :-
 Nifedipine
 Felodipine
 Amlodipine
 Nitrendipine

4. Potassium Channel Opener  Nicorandil

5. Others  Dipyridamole
 Trimetazidine
 Ranolazine
 Ivabradine
 Oxyphedrine

ANTIPLATELET DRUGS :- These are drugs which interfere with platelet function and are useful in the prophylaxis
of thromboembolic disorders. E.g, Aspirin, Ticlopidine, Sulfinpyrazone, Clopidogrel.

10 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


HYPOLIPIDAEMIC DRUGS

These are drugs which lower the levels of lipids and lipoproteins in blood.

The hypolipidaemic drugs have attracted considerable attention because of their potential to prevent cardiovascular
disease by retarding the accelerated atherosclerosis in hyperlipidaemic individuals.

Classification:-

1. HMG-CoA reductase inhibitors (Statins)  Lovastatin


 Simvastatin
 Pravastatin,
 Atorvastatin
 Rosuvastatin
 Pitavastatin

2. Bile acid sequestrants (Resins)  Cholestyramine


 Colestipol

3. Lipoprotein lipase activators  Clofibrate


 Gemfibrozil
 Bezafibrate
 Fenofibrate

4. Lipolysis and triglyceride synthesis inhibitor  Nicotinic acid

5. Others  Ezetimibe
 Gugulipid

HAEMOPOETICS :- are substances required in the formation of blood and are used for treatment of Anaemias.

COAGULANTS :- These are substances which promote coagulation and are indicated in haemorrhagic states.

Fresh whole blood or plasma provide all the factors needed for coagulation and are the best therapy for deficiency
of any clotting factor; also they act immediately. Other drugs used to restore haemostasis are :-

1. Vitamin K
K1 (from plants, fat-soluble)
K3 (synthetic) (i) Fat-soluble :- Menadione (ii)Water-soluble :- Menadione sod. Bisulfite

2. Miscellaneous
Fibrinogen (human), Antihaemophilic factor, Desmopressin, Adrenochrome monosemicarbazone, Rutin, Ethamsylate

11 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


BRONCHODIALATORES
These are the agents used to relax smooth muscles of bronchioles. They should be used only when an element of
bronchoconstriction is present and not routinely.

Classification:-

1. β2 Sympathomietics  Salbutamol
 Terbutaline
β 2 receptor stimulation  Bambuterol
 Salmeterol
increased cAMP formation
 Formoterol
in bronchial muscle cell
They are fastest acting bronchodilators when inhaled.
relaxation
They should be coutiously used in hypertensives & heart patients.

2. Methylxanthines  Theophylline (anhydrous)


 Aminophylline
Three actions:-  Doxophylline
 Choline theophyllinate
Release of Ca2+ from sarcoplasmic reticulum  Hydroxyethyl theophylline
Inhibition of phosphodiesterase (PDE)
They have been extensively used in asthma but not considered as a first
Blockade of adenosine receptors line drugs any more.

3. Anticholinergics  Ipratropium bromide


 Tiotropium bromide
Atropinic drugs cause bronchodilatation by
blocking cholinergic constrictor tone; act
primarily in the larger airways.

 Salbutamol (ASTHALIN, DERIHALER – 100µg metered dose inhaler)


 Terbutaline (TERBUTALINE, BRICAREX - 2.5-5mg tab., 3mg/5ml syrup, 0.5mg/ml inj.)
 Aminophylline (AMINOPHYLLINE - 100mg tab.,250mg/10ml inj.)
 Hydroxyethyl theophylline (DERIPHYLLIN – 100mg tab., 250mg/2ml inj.)

AEROSOLS / INHALANTS :- is a colloid system in which solid or liquid particles are suspended in a gas especially a
suspension of a drug or other substance to be dispensed in a fine spray or mist. E.g, ASTHALIN.

Four classes of antiasthma drugs are available for inhalational use, viz. β2 agonists, anticholinergics, cromoglycate
& glucocorticoids. They are aimed at delivering the drug to the site of action so that lower dose is needed &
systemic side effects are minimized. Faster action of bronchodilators can be achieved compared to oral
administration. Most asthma patients are now maintained on inhaled medication only.

Aerosols are of two types :- (i) use drug in solution :- pressurized metered dose inhaler (pMDI), nebulizers
(ii) use drug as dry powder :- spinhaler, rotahaler

12 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


EXPECTORANTS

These are drugs which increase bronchial secretion or reduce its viscosity, facilating its removal by coughing.

Classification:-

1. Bronchial secretion enhancers  Sodium or Potassium citrate


 Potassium iodide
 Guaiphenesin (Glyceryl guaiacolate)
 Balsum of Tolu
 Vasaka
 Ammonium chloride

2. Mucolytics  Bromhexine
 Ambroxol
 Acetyl cysteine
 Carbocisteine

Bronchial secretion enhancers

Sodium and potassium citrate are considered to increase bronchial secretion by salt action.

Potassium iodide is secreted by bronchial glands and can irritate the airway mucosa. Prolonged use can affect
thyroid function and produce iodism. It is not used now.

Guaiphenesin, vasaka, tolu balsum are plant products which are supposed to enhance bronchial secretion and
mucociliary function while being secreted by tracheobronchial glands.

Ammonium salts are nauseating—reflexly increase respiratory secretions.

Mucolytics

Bromhexine A derivative of the alkaloid vasicine obtained from Adhatoda vasica (Vasaka), is a potent mucolytic and
mucokinetic, capable of inducing thin copious bronchial secretion.
Dose:- adults 8mg TDS, children 1–5 years 4mg BD, 5–10 years 4mg TDS.
BROMHEXINE 8mg tablet, 4 mg/5 ml elixir.

Ambroxol A metabolite of bromhexine having similar mucolytic action, uses and side effects.
Dose:- 15–30mg TDS.
AMBRIL, AMBROLITE, AMBRODIL, MUCOLITE 30 mg tab, 30 mg/5ml liquid, 7.5mg/ml drops.

Acetylcysteine It opens disulfide bonds in mucoproteins present in sputum—makes it less viscid, but has to be
administered directly into the respiratory tract.
MUCOMIX 200mg/ml inj in 1,2,5 ml amps; injectable solution may be nebulized/instilled through trachiostomy tube.

Carbocisteine liquefies viscid sputum in the same way as acetylcysteine and is administered orally (250–750mg TDS).
MUCODYNE 375 mg cap, 250 mg/5 ml syr.

13 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


DIGESTANTS
These are substances intended to promote digestion of food. A number of proteolytic, amylolytic and lipolytic
enzymes are marketed in combination formulations and are vigorously promoted for dyspeptic symptoms, and as
appetite stimulants or health tonics.

They are occasionally beneficial, only when elaboration of enzymes in G.I.T. is deficient. Their routine use in tonics
and appetite improving mixtures is irrational.

1. Pepsin May be used along with HCl in gastric achylia due to atrophic gastritis, gastric carcinoma, pernicious
anaemia, etc.

2. Papain It is a proteolytic enzyme obtained from raw papaya. Its efficacy after oral ingestion is doubtful.

3. Pancreatin It is a mixture of pancreatic enzymes obtained from hog and pig pancreas. It contains amylase, trypsin
and lipase.

4. Diastase and Takadiastase These are amylolytic enzymes obtained from the fungus Aspergillus oryzae.

Preparations:-

DIGEPLEX (Diastase 62.5 mg, pepsin 20 mg per 10 ml after dissolving the tablet in sorbitol base provided)

DIZEC (Pancreatin 250 mg, sod. Tauroglycocholate 50 mg, Methyl polysiloxane 25 mg tab.)

DIMOL (40 mg tab. single ingredient – Methyl polysiloxane)

CARMINATIVES
These are drugs which promote the explusion of gases from the G.I.T. and give a feeling of warmth & comfort in the
epigastrium.

Commonly used drugs are :-

 Sodium bicarbonate (0.6 – 1.5 g.)


 Oil peppermint (0.06 – 0.1 ml)
 Tincture cardamom (1 – 2 ml)
 Oil of dil (0.06 – 0.2 ml)
 Tincture ginger (0.6 – 1 ml)

Sodium bicarbonate reacts with gastric HCL & envolves CO2 which rapidly distands stomach, relaxes LES & brings
about erructation.

The others are condiments and spices, contain volatile oil, which by their mild irritant action & flavour relax LES &
increase G.I.T. motility.

Used for :- flatulent dyspepsia

(LES Lower Esophageal Sphincter)

14 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


ANTI-ULCER
Anti-ulcer drugs are those which are effective in the treatment of peptic ulcer either reduce/ neutralize gastric acid
or increase mucosal resistance to acid pepsin attack & protects and heals the ulcer surface or are anti H.pyroli
bacteria.

Peptic ulcer (especially duodenal) is a chronic remitting and relapsing disease lasting several years. The goals of
antiulcer therapy are :-
• Relief of pain
• Ulcer healing
• Prevention of complications (bleeding, perforation)
• Prevention of relapse.

Classification:-

1. Reduction Of Gastric Acid Secretion (i) H2 antihistamines


 Cimetidine
 Ranitidine
 Famotidine
 Roxatidine

(ii) Proton pump inhibitors


 Omeprazole
 Esomeprazole
 Lansoprazole
 Pantoprazole
 Rabeprazole

(iii) Anticholinergic drugs


 Propantheline
 Oxyphenonium
 Pirenzepine

(iv) Prostaglandin analogue


 Misoprostol

2. Neutralization Of Gastric Acid (ANTACIDS) (i) Systemic


 Sodium bicarbonate,
 Sodium citrate

(ii) Nonsystemic
 Magnesium hydroxide
 Aluminium hydroxide
 Calcium carbonate

3. Ulcer Protectives  Sucralfate

4. Anti-H. Pylori  Amoxicillin


 Metronidazole
 Tinidazole

15 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


LAXATIVES
These are drugs that promote evacuation of bowels.

(a) Laxative or aperient :- milder action, elimination of soft but formed stools.
(b) Purgative or cathartic :- stronger action resulting in more fluid evacuation.

Many drugs in low doses act as laxative and in larger doses as purgative.

Classification:-

1. Bulk forming Dietary fibre :-


 Bran
 Psyllium (Plantago)
 Ispaghula
 Methylcellulose

2. Stool softener  Docusates (DOSS)


 Liquid paraffin

3. Stimulant purgatives (i) Diphenylmethanes


 Phenolphthalein
 Bisacodyl
 Sodium picosulfate

(ii) Anthraquinones (Emodins)


 Senna
 Cascara sagrada

(iii) 5-HT4 agonist


 Prucalopride

(iv) Fixed oil


 Castor oil

4. Osmotic purgatives  Magnesium salts :- sulfate, hydroxide


 Sodium salts :- sulfate, phosphate
 Lactulose

Psyllium & Ispaghula (ISOGEL- 27g./ 30g., FYBOGEL 3.5g./ 5.4g. powder)

Docusates (LAXICON 100mg tab.; 125mg/50ml enema, DOSLAX 150mg cap.)

Bisacodyl (DULCOLAX 5mg tab.)

Sodium picosulfate (LAXICARE, CREMALAX 10mg tab.)

Senna (GLAXENNA, SOFSENNA 12mg tab.)

AGAROL (liquid paraffin 9.5ml, phenophthalein 400mg, agar 60mg / 30ml emulsion)

16 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


Type of stools and latency of action of purgatives employed in usually recommended doses

Soft, formed faeces (take 1–3 days) Semifluid stools (take 6–8 hrs) Watery evacuation (take 6–8 hrs)
 Bulk forming  Phenolphthalein  Saline purgatives
 Docusates  Bisacodyl  Castor oil
 Liquid paraffin  Sod. Picosulfate
 Lactulose  Senna

Mechanism of action :-

All purgatives increase the water content of the faeces by :-

(a) A hydrophilic or osmotic action, retaining water and electrolytes in the intestinal lumen—increase volume of
colonic content and make it easily propelled.

(b) Acting on intestinal mucosa, decrease net absorption of water and electrolyte; intestinal transit is enhanced
indirectly by the fluid bulk.

(c) Increasing propulsive activity as primary action—allowing less time for absorption of salt and water as a
secondary effect.

Purgative abuse :-

Some individuals are obsessed with using purgatives regularly. This may be the reflection of a psychological problem.
Others use a purgative casually, obtain thorough bowel evacuation, and by the time the colon fills up for a proper
motion (2–3 days) they get convinced that they are constipated and start taking the drug regularly. Chronic use of
purgatives must be discouraged. Once the purgative habit forms, it is difficult to break. Dangers of purgative abuse
are:

1. Flairing of intestinal pathology, rupture of inflamed appendix.


2. Fluid and electrolyte imbalance, especially hypokalaemia.
3. Steatorrhoea, malabsorption syndrome.
4. Protein losing enteropathy.
5. Spastic colitis.

17 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


ANTI-DIARRHOEALS
These are the agents useful in the management of diarrhoea.

Diarrhoea is too frequent, often too precipitate passage of poorly formed stools. It is defined by WHO as 3 or more loose or
watery stools in a 24 hour period. In pathological terms, it occurs due to passage of excess water in faeces.This may be due to:-

• Decreased electrolyte and water absorption.


• Increased secretion by intestinal mucosa.
• Increased luminal osmotic load.
• Inflammation of mucosa and exudation into lumen.

Principles of management :-

1. Rehydration (i) IV rehydration :- When fluid loss is severe i.e, >10% of


body weight.
New formula WHO-ORS Total osmolarity 245 mOsm/L
Content Concentrations
NaCl : 2.6 g Na+ — 75 mM
(ii) Oral rehydration :- When fluid loss is mild.
KCl : 1.5 g K+ — 20 mM
Trisod. citrate : 2.9 g Cl¯ — 65 mM (available as ORETRAL-A, ELECTROBION, ELECTRAL 21 g sachet for
Glucose : 13.5 g Citrate — 10 mM 1000 ml; WALYTE, RELYTE 4.2 g sachet for 200 ml)
Water : 1 L Glucose — 75 mM

2. Maintenance Of Nutrition Contrary to traditional view, patients of diarrhoea should not be


starved. Fasting decreases brush border disaccharidase enzymes &
reduces absorption of salt, water & nutrients; may lead to
malnutrition if diarrhoea is prolonged or recurrent.

Feeding during diarrhoea has been shown to increase intestinal


digestive enzymes and cell proliferation in mucosa.

Simple foods like breast milk or ½ strength buffalo milk, boiled


potato, rice, chicken soup, banana, sago, etc. should be given as soon
as the patient can eat.

3. Drug Therapy

(i) Specific antimicrobial drugs (ii) Non-specific anti-diarrhoeal drugs


A. Antimicrobials are of no value In diarrhoea due to
noninfective causes, such as :- Class Drug Use
 Irritable bowel syndrome (IBS) Absorbants Ispaghula Irritable bowel syndrom
(IBS)
 Coeliac disease Psyllium
Methyl cellulose Ileostomy diarrhoea
 Pancreatic enzyme deficiency
Colostomy diarrhoea
 Thyrotoxicosis
Antisecretory Sulfasalazine Ulceritive colitis
B. Antimicrobials are useful only in severe disease (but not in Mesalazine Inflammatory bowel
diseases (IBD)
mild cases) :- Atropine
Octreotide Travellers’ diarrhoea
 Travellers’ diarrhoea Diarrhoea in AIDS
 Shigella enteritis Racecadotril
Acute secretory
 Nontyphoid Salmonella diarrhoea
 Yersinia enterocolitica
Antimotility Codein Travellers’ diarrhoea
C. Antimicrobials are regularly useful in :- Loperamide Idiopathic diarrhoea
 Cholera Diphenoxylate After anal surgery,
 Clostridium difficile colostomy
 Amoebiasis

18 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


ANTI-EMETICS
These are drugs used to prevent or suppress vomiting.

Vomiting occurs due to stimulation of the emetic (vomiting) centre situated in the medulla oblongata. Multiple
pathways can elicit vomiting.

Classification:-

1. Anticholinergics  Hyoscine
 Dicyclomine

2. H1 antihistaminics  Promethazine
 Diphenhydramine
 Dimenhydrinate
 Doxylamine
 Meclozine (Meclizine)
 Cinnarizine

3. Neuroleptics (D2 blockers)  Chlorpromazine


 Triflupromazine
 Prochlorperazine
 Haloperidol

4. Prokinetic drugs  Metoclopramide


 Domperidone
 Cisapride
 Mosapride
 Itopride

5. 5-HT3 antagonists  Ondansetron


 Granisetron
 Palonosetron
 Ramosetron

6. Adjuvant antiemetics  Dexamethasone


 Benzodiazepines
 Dronabinol
 Nabilone

Doxylamine (DOXINATE, VOMNEX, NOSIC 10mg with pyridoxine 10mg tab.)

Domperidone (DOMSTAL, DOMPERON, NORMETIC 10mg tab.; 1mg/ml syrup)

Ondansetron (EMSET, OSETRON, EMSETRON 4,8mg tabs.; 2mg/ml inj. In 2ml & 4ml amps.)

Granisetron (GRANICIP, GRANISET 1mg,2mg tabs; 1mg/ml inj. In 1ml & 3ml amps.)

19 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


HEPATOPROTECTIVES

These are the agents usefull for prevention & treatment of hepatic diseases.

Prevention :-

Some but not all liver disease can be prevented by,


 Vaccination- hep.A & B
 Practicing good hygine
 Avoiding drinking
 Practicing safe sexual practice
 Avoiding toxic substances
 Proper use of medicines
 Well balanced food intake

Treatments :-

 Anti-hepatotoxic
 Hepatotropic
 Hepatoprotective

Usefull herbs :-

 Bhringraja (Eclipta alba)


 Yastimadhu (Glycyrrhiza glabra)
 Punarnava (Boerhavia diffusa)
 Apamarga (Achyranthus aspera)
 Kiratatikta (Swertia chirata)

Marketed formulatons :-

 LIV-52
 LIMARIN

20 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


DIURETICS

Diuretics are the drugs which increase the urine formation together with natriuresis. E.g, Furosemide, Thiazides

Only a few drugs produce diuresis by increasing GFR, and these are relatively weak in action. Most of the diuretics
used to therapeutically act by interfering with sodium re-absorption by the tubules.

Classification :-

1. Thiazide diuretics  Chlorothiazide


 Chlorthalidone
 Hydrochlorothiazide
 Indapamide

2. Loop diuretics  Torsemide


 Furosemide
 Bumetanide

3. Potassium-sparing diuretics  Amiloride


 Triamterene
 Eplerenone

Usefull in :-

 CHF (Congestive Heart Failure)


 Odema
 High blood pressure
 Arrhythmia

Most common side effects :-

 Headache
 Dizziness
 Thirst
 Gout
 Diarrhoea
 Skin rashes
 Muscle cramps
 Kidney failure

21 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


ANTI-DIURETICS

These are drugs that reduce urine volume particularly in diabetes insipidus.

Classification :-

1. Antidiuretic hormone (ADH-Vasopressin)  Desmopressin


 Lypressin
 Terlipressin

2. Thiazide diuretics  Amiloride

3. Miscellaneous  Indomethacin
 Chlorpropamide
 Carbamazepine

USES :-

 Diabetes insipidus
 Bedwetting in children & nocturia in adults
 Renal concentration test
 Haemophillia
 Before abdominal radiography

LITHOTRIPTICS :- These are the drugs which break down the calculi either renal or ureteric.

In modern pharmacology there are no substances that have lithotriptic capebility & are harmless to the patients.

Some Ayurvedic formulations having lithotriptic action :-

 Shweta parpati
 Palash kshara
 Goksuradi guggulu
 Pashanbheda churna

22 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


HORMONAL THERAPY

When hormones are used as therapy in various condition, it is called as hormonal therapy.

Hormon is a substance secreted by specialised cells and transported to a distant site to exert its action.

Hormones for clinical uses may obtain from natural sources (animal glands) or may be prepared synthetically. As well
as their synthetic analogues are used as a drug and it is called as hormonal therapy.

Synthetic analogues may have the advantages because of it is abundantly available and cheaper e.g. Prednisolone.

They are Mainly secreted by endocrine glands :-

 Hypothalamus
 Pitutary
 Thyroid
 Adrenal
 Gonads etc.

Grouping of hormons :-

1. Amino acid derivatives Catecholamines, Dopamine, Thyroid Hormones


2. Peptides Hypothalamic Regulatory Hormones (TRH, Gnrh, CRH), Vasopressin, Somatostatin
3. Proteins Insulin, GH, PTH
4. Steroids Adrenocortical And Gonadal Sterois
5. Vitamin derived Vit. D Derivatives, Retinoids

Mechanism of action :-

Hormones act through specific receptors. Receptors divided in 2 classes.

a) Cell membrane receptors :- Amino Acid Derivatives, Peptides.


b) Nuclear receptors :- Steroidal, Vitamin, Thyroid Hormones.

Uses :-

1) For diagnosis purpose:


 ACTH used for diagnosis of addison’s disease
 Dexamethasone is used for diagnosis of cushing’s syndrome.

2) For therapeutic purpose:


 As replacement therapy: E.g. insulin in diabetes, throxine in hypothyrodism etc.
 As pharmacotherapy: e.g. glucocorticoids in asthma

23 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


ANTI-OBESITY
An anoretic drugs can help the obese to tolerate a reducing diet for short periods. These should be taken only in
severe obesity but not for cosmetic reason in mild to modrate obesity.

Classification :-

1. Centrally Acting Appetite Suppressant (Anorexiants) (i) Adrenergic agents


 Ampheramine
 Mepheteramine
 Mazindol

(ii) 5-HT antagonist


 Fenfluramine
 Dexfenfluramine
 Fluoxentine

(iii) Both
 Sibutramine

(iv) Cannabinoid receptor antagonist


 Rimonabant

2. Drugs Acting In The GI Track (i) Bulk anorexiants


 Dietary fiber
 Methylcellulose
 Guar gum
 Karaya gum

(ii) Non absorbable fat substitutes


 Olestra

(iii) Lipase inhibitor


 Orlistat

3. Miscellaneous: Biguanides (i) Bulk anorexients


non digestable pollysaccharide, when injested sweels and
adds to the bulk in the diet. So it used as appetite satiator.
Not more effective than high residue low calorie diet.

(ii) Digestion inhibitors


Olestra: mixture of sucrose fatty acid which neither digest
nor absorbed in GI tract. It increase bowel function and
stool bulk. Recommended as fat substitute in cooking.
Orlistat: inhibit the lipase and not absorbed in GIT, inhibit
the fat absorption as well as reduces the plasma
cholesterol level.

24 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


ANTI-DIABETICS
These are the agents usefull in management of diabitis.

Classification of oral hypoglycemic :-

1. Sulfonylureas  Tobutamide
 Chlorpropamide
 Glipizide
 Glibenclemide
 Glimipride

2. Biguanides  Metformin
 Phenformin

3. Meglitinide  Repaglinide
 Nateglinide

4. Thiazolidinediones  Rosiglitazones
 Pioglitazones

5. α glucosidase inhibitors  Acrobose


 Miglitol

Mechanism of action of oral hypoglycemic drugs :-

 Stimulators of insulin release by beta cells :- Sulfonylureas, Meglitinides


 Inhibitors of hepatic gluconeogenesis :- Bigunides
 Reduce insulin resistance :- Glitazones
 Inhibitors of dipeptidyl dipeptidase-4 :- Sitagliptin

Side effects :-

 Weight gain
 Hypoglycemia
 Allergic reaction
 Liver diseases
 Cardio vascular symptoms

25 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


ANTI-THYROID
Conventionally only the synthesis inhibitors are called antithyroid drugs, though this has also been applied to all
thyroid inhibitors.

Thyroid gland hormones :-

 Thyroxine (T4)
 Triiodothyronine (T3)
 Calcitonin
Regulated by pitutary (TSH) and hypothalamus (TRH)

Thyroid inhibitors :- These drugs used to lower the functional capacity of the hyperactive thyroid gland.

Classification of thyroid inhibitors :-

1. Inhibit hormone synthesis (Antithyroid Drugs)  Propylthiouracil


 Methimazole
 Carbamizole

2. Inhibit iodide trapping (Ionic Inhibitors)  Thiocyanates


 Perchlorates
 Nitrates

3. Inhibit hormone release  Iodine


 Iodides of Na and K
 Organic iodide

4. Destroy thyroid tissue  Radioactive iodine (131I, 125I, 123I)

Mechanism:- It penetrates cells by active transport and produce majority of their actions by combining with a
nuclear thyroid hormone receptors.

Therapeutic uses :-
 Thyrotoxicosis
 Toxic nodular goiter

Adverse effect :-
 Hypothyroidism
 Goiter
 G.I. intolerence
 Skin rashes
 Joint pain
 Loss of taste
 Fever
 Liver damage

26 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


OXYTOCICS

It is called as uterine stimulants or abortificients or oxitocics. These drugs increase uterine motility especially at term.

Classification :-

1. Posterior pituitary hormones  Oxytocin


 Desamino Oxytocin

2. Ergot alkaloids  Ergometrine


 Methylergometrine

3. Prostaglandins  Pge2
 Pgf2α
 Misoprostol

4. Miscellaneous  Ethacradine
 Quinine

Mechanism of action :- through receptors.

Therapeutic uses :-
 Induction of labour
 Uterine inertia
 Postpartum hemorrhage
 Cesarean section
 Breast engorgement

GALACTAGOGUES :- are the substances that can help to increase breast milk supply. Prolactin is a woman’s
main breastmilk producing hormone.

Examples,
 Domperidone
 Metoclopramide
 Chlorpromazine
 Oxytocin
 Foods such as, Carrot Seeds, Beet Leaves, Spinach, Plain Oats etc.

27 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


CONTRACEPTIVES

Drugs that used for reversible suppression of fertility is called as contraceptives.

Methods :-
1. Chemical:- Hormonal therapy
2. Mechanical:- IUCD etc.

Fertility can be controlled by using drugs which can act by,

 Inhibiting ovulation
 Modifying the cervical mucous
 Interfering with implantation
 Slowing down the rate of egg transport
 Preventing the ovum maturation and sperm capacitating
 Immunological methods
 Inhibiting the spermatogenesis in male

Classification of OCP (oral contraceptive pills) :-

1. Combined pill Dose: 1 tablet daily for 21 days at bed time on 5th day to 25th day of cycle in
28 day cycle. The next course is started after 7 days of last dose.
Contains an estrogen and a progestin Mechanism: inhibiting secretion of FSH and LH by estrogen and progestine
respectively. As a result follicle fail to develop and fail to rupture thus ovulation
does not occur.
This is most popular and most effective method now days.
e.g.
1. MALA-D: norgestrel (0.3mg) + ethynil estradiol (30 µg)
2. OVARAL: levonorgestrel (0.15 mg) + ethynil estradiol (50 µg)

2. Phased regimens The estrogen dose is kept constant (30-40 µg), While the amount of
progestin is low in the first phase and progressively higher in the second and
These are biphasic or triphasic third phase.
It is particularly prescribed recommended for women over 35 years.
Mechanism same as combined pills.

3. Minipill (progestin only pill) Mechanism: cervical mucous secretion is hostile to sperm penetration is
evoked by progestin.
If ovulation occurs blastocyst may fail to implant because endometrium is
Low dose of progestin is taken daily either hyper proliferative or hyper secretory or atrophic.
Uterine and tubal contraction may be modified to disfavor fertilisation.
Ex. OVERETTE: norgestrel (75µg)
It is Less popular method

4. Postcoital contraception Dose: after coitus as early as possible but within 72 hrs.
Mechanism: they dislodge a just implanted blasocyst or may interfere with
Used to prevent unexpected or accidental fertilisation and implantation.
exposure (rape etc.) only Ex.
1. I-PILL: levonorgestrel (1.5 mg): twice with 12 hrs gap
2. OVARAL: levonorgestrel (0.25 mg) + ethynil estradiol (50 µg): twice with 12
hrs gap
3. MEFEPRISTONE: 600mg single dose

28 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


Injectable contraceptives classification :-

 Long acting progestin alone: injecting once/2-3 months


ex. Northisterone enanthat
depot medroxyprogesterone acetate

 Long acting progestin+ long acting estrogens: once/ month


Ex. MPA + estradiol

Implants :-
These drug delivery systems implanted under the skin, from which drug is released slowly over a period of 1-5 years.

Side effects :-

Nonserious:
 Nausea and vomiting
 Headache
 Breakthrough bleeding or spotting
 Breast discomfort

Later side effects:


 Weight gain
 increase body hair
 Chloasma (pigmentation)
 Pruritis vulvae
 Carbohydrate intolerance- diabetes, Mood swings, abdominal distension

Serious complications:
 Leg vein and pulmonary thrombosis
 Coronary and cerebral thrombosis
 Rise in blood pressure
 Genital carcinoma
 Benign hepatomas

Male contraceptives

No satisfactory medicine because of:


 Complete suppression is difficult without affecting other tissue.
 Spermatogenesis takes 64 days
 Gonadotropin inhibition suppresses testosterone resulting loss of libido and infertility.

STYPTICS :- Substances used to stop bleeding from a local and approchable site by causing contraction of body
tissues and canals. Used by oozing surfaces like, tooth socket, open wound etc. They should never be injected.

Thrombin :- used in haemophilia, neurosurgery, skin grafting.


Fibrin :- used as a sheets or foam for covering or packing bleeding surface.
Gelatine foam :- used for packing wounds.
Vasoconstrictors , Astringents like tannic acid etc.

29 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


ANTI-HISTAMINE

These drugs antagonize actions of histamine. They are used in allergies, cold, cough etc.

Classification :-

A) H1 antihistaminics

1. Highly sedative  Diphenhydramine


 Dimenhydrinate
 Promethazine
 Hydroxyzine

2. Moderately sedative  Pheniramine


 Cyproheptadine
 Buclizine
 Cinnarizine

3. Mild sedative  Chlorpheniramine


 Dexchlorpheniramine
 Cyclizine
 Triprolidine
 Clemastine

4. Second generation drugs  Loratadine


 Cetrizine
 Levocetrizine
 Misolastine
 Ebastine
 Rupatadine

B) H2 antagonist The first H2 blocker Burimamide was developed by Black in 1972. Metiamide was the next, but both
were not found suitable for clinical use. Cimetidine was introduced in 1977 and gained wide usage. Ranitidine,
famotidine, roxatidine, and many others have been added subsequently. They are primarily used in peptic ulcer,
gastroesophageal reflux and other gastric hypersecretory states.

C) H3 antagonist Though some selective H3 antagonists have been produced, they have not found any clinical utility.

30 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


ANTI-MICROBIAL

An antimicrobial is an agent that kills microorganisms (Bactericidal) or inhibits their growth (bacteriostatic).

Antimicrobial medicines can be grouped according to the microorganisms they act primarily against. For example,
antibacterials are used against bacteria and antifungals are used against fungi.

The use of antimicrobial medicines to treat infection is known as antimicrobial chemotherapy, while the use of
antimicrobial medicines to prevent infection is known as antimicrobial prophylaxis.

Classification :-
(Types of organisms against which primarily active)

1. Antibacterial • Penicillins
• Aminoglycosides
• Erythromycin

2. Antifungal • Griseofulvin
• Amphotericin B
• Ketoconazole

3. Antiviral • Acyclovir
• Amantadine
• Zidovudine

4. Antiprotozoal • Chloroquine
• Pyrimethamine
• Metronidazole
• Diloxanide

5. Anthelmintic • Mebendazole
• Pyrantel
• Niclosamide
• Diethyl carbamazine

Mechanism of action :-

Antimicrobial drug may act by destroying the organism or by inhibiting growth. The selective toxic action on the
infecting organism is the key to beneficial actions of antibiotics.

These drugs can hit multiple targets in bacteria

• Interference with cell wall synthesis


• Damage to the cytoplastic membrane
• Inhibition of protein synthesis and impairment of function of the ribosome
• Interference with transcription/translation of genetic information
• Antimetabolite action
• Inhibition of viral enzymes
31 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17
Side effects :-

• Development of allergic and anaphylactic reaction


• Selective toxicity: nephrotoxicity
• Development of superinfection
• Multiple drug resistant organism
• Deficiency of certain vitamins
• Fetal damage
• False sense of security in the patient and physician

Choice of an antimicrobial agent :-

 Selection of antomicrobial agent: host related factors

• Age of the patient: chloramphenicol may cause serious toxic effects in infants
• Pregnancy and neonatal period: Penicillins, Cephalosporins, Erythromycin, Linomycin, Clindamycin,
Azithromycin, INH, Ethambutol can be safely given in pregnancy others used when must.
• Immunocompetency status of the patient
• Severity of the infection
• History of previous allergic reaction

 Selection of antomicrobial agent: pathogen related factors

• The probable causative organism and the expected clinical course of the infection
• Identification of the causative micro-organism and its severity to anti microbial drugs
• Possibility of drug reaction

 Selection of antomicrobial agent: drug related factors

• Nature of the drug


• Risk of drug toxicity
• Cost of the therapy
• Pharmaco kinetic property of the drug
• Probability of drug compliance by the patient

32 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


ANTI-BIOTICS
These are substances produced by micro-organisms which selectively suppress or kill other micro-organisms at very
low cone.

Classification :-

A) Acc. to their spectra,

1. Mainly effective against gram-positive bacteria (i) Penicillins


• Penicillin G
Useful in infections like pneumococcal (pneumonia), streptococcal (meningitis • Penicillin V
etc), gonococcus (gonorrhoea), treponima palidum (syphilis), clostridium • Ampicillin
tetany (tetany) etc. • Dicloxacillin

(ii) Macrolides
• Erythromycin
• Azithromycin

(iii) Lincosamide
• Licomycin
• Clindamycin

2. Mainly effective against gram negative bacteria (i) Aminoglycosides


• Streptomycin
Useful in infections like urinary tract infection, peritonitis, meningitis, • Gentamicin
osteomyelitis, septic burns, otitis, septicemia etc. • Amikacin
• Neomycin

(ii) Non amino glycosides


• Colistin
• Spectinomycin

3. Effective against both gram positive and • Ampicillin


negative bacteria • Amoxycillin
• Ceftriaxone
• Cefpodoxime

4. Effective against both gram positive and Tetracyclines


negative bacteria, rickettsiae and chlamydia • Doxycycline
• Minocycline
(broad spectrum)
5. Effective against acid fast bacilli • INH (Isonicotinic acid Hydrazide)
• Streptomycin
Useful in treatment of tuberculosis. • Viomycin

6. Effective against fungi • Nystatin


• Amphotericin B
Useful in fungal infections like candidiasis of vagina, mouth, skin and gut, • Griseofulvin
ringworm, tinea, onycomyosis etc.

7. Effective against protozoa • Paromomycin


• Tetracyclines
Useful in protozoal infections.

8. Antimalignancy antibiotics • Actinomycin D


• Mitomycin
Useful in certain types of cancer

33 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


B) Acc. to Chemical structure,

1. Sulfonamides and related group • Sulfadiazine

2. Diaminopyrimidines • Trimethoprim
• Pyrimethamine

3. Quinolones • Norfloxacin
• Ciprofloxacin

4. β lactum antibiotics • Penicillins


• Cephalosporins

5. Tetracyclines • Tertracyclin
• Doxicycline

6. Nitrobenzene derivatives • Chloramphanicol

7. Aminoglycosides • Streptomycine
• Gentamycin
• Amikacin

8. Macrolide antibioitics • Erythromycin


• Azithromycin

9. Lincosamide antibiotics • Lincomycin


• Clindamycin

10. Glycopeptide • Vancomycin

11. Oxazolidinone • Linezoid

12. Polypeptide antibiotics • Polymixin B


• Colistin

13. Nitrofuran derivatives • Nitrofurantoin

14. Nitromidazoles • Metronidazole


• Tinidazole

15. Nicotinic acid derivatives • Isoniazide


• Pyrazinamide

16. Polyene antibiotics • Nystanin


• Amphotericin B

17. Azole drivatives • Fluconazole


• Clotrimazole
• Ketoconazole

18. Others • Rifampicin


• Spectinomyocin
• Viomycin
• Ethambutol
• Griseofulvin

34 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


ANTI-MALARIAL

These are drugs used for prophylaxis, treatment and prevention of relapses of malaria.

Malaria caused by 4 types of the protozoal parasite plasmodium.

• P. malariae
• P.oval
• P.vivex
• P.falsiperum

Pathology :-

Mechanisms :-

 Casual prophylaxis :- These drugs prevent the maturation of or destroy the sporozites within the infected
hepatic cells. Eg. Primaquine

 Suppressives :- These drugs inhibit erythrocytic schizogony and prevent the rupture of the infected
erythrocytes. Eg. Quinine, artimisine

 Radical curatives :- Total eradication of erythrocytic and exoerythrocytic schizogony eg. Primaquine in
p.vivax

 Gametocidal :- Elimination of the male and female gametes of plasmodia formed in the blood. Gametocidal
action is of no benefit to the patient being treated but will reduce the transmission of the mosquito.

35 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


Classification :-

1. 4-Aminoquinolines  Chloroquine
 Amodiaquine
 Piperaquine

2. Quinoline-methanol  Mefloquine

3. Cinchona alkaloid  Quinine


 Quinidine

4. Biguanides  Proguanil (Chloroguanide)


 Chlorproguanil

5. Diaminopyrimidines  Pyrimethamine

6. 8- aminoquinololes  Primaquine
 Bulaquine

7. Tetracyclines  Tetracycline
 Doxicycline

8. Sesquiterpine lactones  Artesunate


 Artemether
 Arteether

9. Amino alcohols  Halofantrine


 Lumefantrine

10. Mannich base  Pyronaridine

11. Naphthoquinone  Atovaquone

36 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


AMOEBICIDAL
These are drugs useful in infection caused by the anaerobic protozoa Entamoeba histolytica.

Classification :-

1. Tissue amoebicides (i) For both intestinal and extraintestinal amoebiasis

Nitroimidazoles
 Metronidazole
 Tinidazole
 Secnidazole
 Ornidazole
 Satranidazole

Alkaloids
 Emetine
 Dehydroemetine

(ii) For extraintestinal amoebiasis only:

 Chloroquine

2. Luminal amoebicides (i) Amide


 Diloxanide furoate
 Nitazoxanide

(ii) 8-Hydroxyquinolines
 Quiniodochlor (Iodochlorohydroxyquin, Clioquinol)
 Diiodohydroxyquin (Iodoquinol)

(iii) Antibiotics
 Tetracyclines
 Paromomycin

ANTI-FILARIAL :- These are drugs used for the cure and prevention of filariasis.
E.g, Diethylcarbamazine, Ivermectin.

ANTHELMENTIC :- These are drugs that either kill (vermicide) or expel (vermifuge) infesting helminths.
Exampels,
 Mabendazole (MABEX, WORMIN, MENDAZOLE 100mg tab. ; 100mg/5ml susp. For round worm, hook worm)
 Albendazole (400mg dose, For ascaris, hook worm, trichuris)
 Thiabendazole (an alternative to albandazole; rarely used now)
 Piperazine (For Round worm infection; 4.5g.)
 Levamisole, Tertramisole (TETRAMISOLE, LEVAMISOLE 50,100mg tab.)
 Niclosamide (NICLOSAN, NICLOTAP 0.5g tab. For tap worm)

37 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


ANTI-FUNGAL
These are the drugs used for superficial aand deep (systemic) fungal infections.

Fungal infection occurs as primary and secondary to antibiotic therapy. Individual suffering from malignancy, DM,
those on corticosteroids are more prone to fungal infection.

Classification :-

1. Antibiotics  Greseofulvin
 Nystanin
 Amphotericin B ; Used in tinea capatis, tinea curis

2. Antimetabolites  Flucitosine ; used mainly against yeast infection

3. Azole derivatives  Clotrimazole


 Ketaconazole
 Fluconazole
 Itraconazole

Broad spectrum antifungal used in candidiasis, tinea and other fungal infection.

4. Miscellaneous  Terbinafine
 Benzoic acid

38 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


VITAMINS & MINERALS
A vitamin is an organic substance that is found in food, is not made in the body and is required in small quantities,
usually a cofactor for enzymes.
Some vitamins such as Vitamin K, pantothenic acid, folic acid and cynocobalmin are also synthesized by bacterial
flora of the intestine.

Causes of vitamin deficiency :-

 Deficient diatary intake


 Inadequeate absorption from the GI tract: chronic diarrhoea, malabsorption syndrome, obstructive jaundice,
interference with intestinal flora by oral antibiotics, interference with absorption by drugs like liquid paraffin.
 Interference with utilisation: usually drugs. Eg. Pyrimethemine, trimethoprime, methotraxate which
interference with folic acid utilisation.
 Increased demand: during growth, in pregnancy, during lactation, under stress, in fever and other catabolic
conditions like hyperthyrodism.

Classification:- Vitamis are classified in two groups.


1. Fat soluble :- Vitamin A,D,E,K
2. Water soluble :- Vitamin B complex and C

Fat soluble vitamins

Vit. Chem. name Daily req. Deficiency states Preparations


A Retinol 600 µg  Night blindness AQUASOL-A
 Keratomalacia 50,000 IU cap.; 100,000 IU/2ml inj.
 Psoriasis
AROVIT
 Dermatitis
50,000 IU tab. ; 100,000 IU/2ml inj.
 Bone pain
 Neurological symptoms

D Calciferol 05 µg  Rickets ACRACHOTOL, OSTELIN FORTE


 Osteomalacia 60,000 IU/ml inj. (1ml amp.)
 Hypoparathyroidism
CALCIROL
 Osteoporosis 60,000 IU/g granules

E α Tocopherol 10 mg  Reproductive problems EVION, EPHYNAL


 Myopathy 10mg tab. ; 100mg/2ml inj.
 Neurological problems

K Phytonadione 80 µg  Chronic liver disease SYNKAVIT


 Warfarin over dose 5mg tab. ; 10mg/ml inj.
 Tenderic to bleed
 Prolonged chemotherapy

39 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


Water soluble vitamins

Vit. Chem. name Daily req. Deficiency states Preparations


B1 Thiamine 1.5mg  Beriberi BERIN
 Neuritis 50,100mg tab.; 10mg/ml inj.
 Alcoholic neuritis
BENEURON
5mg cap.

B2 Riboflavin 1-2mg  Glossitis LIPABOL


 Dermatitis 20mg tab.

RIBOFLAVIN
10mg/ml inj.

B3 Niacin 5-20mg  Pellarga NICOTINIC


 Hyper lipidaemia 25,50mg tab.

B6 Pyridoxine 1-3mg  Morning sickness PYRIDOXINE HCL


 Infantile convulsions 50mg/2ml inj. ; 10mg tab.
 Glossitiis
 Stomatitis
 Convulsions

B12 Cobailamine 1-3mg  Megalo blastic anaemia REDISOL, MACRABIN


35µg/ml liq.

Vit. B 12
500, 1000 µg in 10ml vial

C Ascorbic acid 50-60mg  Scurvy CECON


Folic acid (ascorbic acid)  Megalo blastic anaemia 500mg tab.; 100mg/ml drops
 Acidifying urine
100µg CELIN
(folic acid) 50,100 mg tab

FOLVITE
5g tab.

REDOXON
3mg/ml inj.

Minerals

Minerals Daily requirments Deficiency states


Calcium 800-1200mg Rickets, Osteomalcia
Phosphorus 800-1200mg Osteomalacia, CNS symptoms
Magnesium 250-300mg Cardiac arrhythmias
Iron 10-15mg Microcytic anaemia
Zinc 10-15mg Hypogonadism, Skin manifestation
Iodine 150µg Goitre
Selenium 40-60µg Cardiomyopathy

40 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


WATER IMBALANCE & IV FLUIDS

Water :- Water constitues about 60% of the total body weight. ECF (Extra Cellular Fluid) & ICF (Intra Cellular Fluid)
contain aprox 16L to 30L of water respectively. Reduction of water content of ECF results in thirst & release of
antidiuretic hormone from the posterior pitutary, which acts on the renal tubules to enhance absorption of water,
on the other hand any excess of water over the basis requirment is disposed of by normal kidney.

Water excess occurs when large amount of fluid is administered in presence of renal disease with oligouria, results
hypo tonicity of body fluids, leading to cerebral oedema & also oedema affecting other part of body.

Dehydration is condition in which there is depletion of water usually accompanied by the disturbance of electrolytes
metabolism. Common causes for dehydration are,

 Excessive sweating
 Reduces water intake
 Increase loss of water & electrolytes
 Cholera
 Acute diarrhoea
 Deficiency of ADH

Treatment consist of adequate replacement of water & electrolytes orally or by injecting 50% glucose solution IV for
oral rehydration.

New formula WHO-ORS

Content Concentrations
NaCl : 2.6 g Na+ — 75 mM
KCl : 1.5 g K+ — 20 mM
Trisod. citrate : 2.9 g Cl¯ — 65 mM
Glucose : 13.5 g Citrate — 10 mM
Water : 1 L Glucose — 75 mM
Total osmolarity 245 mOsm/L

Electrolytes :- The movement of cations paly major role in the functional activity of cells & they also maintain their
osmotic pressure & the size of their osmotic pressure. The ICF & ECF have different compositions, but equal
osmolarity. The ECF contains mainly Na+ as cation accompanied by anions like Cl-, HCO3 & HPO4. While ICF contains
K+ as cation accompanied by a wide variety of anions, such as HCO3-, PO4, SO4 & citrates.

Active transport in cell membrane continuosly keeps Na+ outside & k+ inside the cell.

1. Sodium balance

A) Hyponatraemia

Causes :-
 Excessive sweating
 Severe GIT disorders
 Renal causes
 Chronic alcoholism, malnutrition, Liver disease
 Psychogenic disorders

41 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


Treatment :- Oral or IV replacement
B) Hypernatraemia

Causes :-
 ECF losses
 Fever
 Vomiting
 Diarrhoea
 Renal losses of water
 Diabetes insipidus
 Acute nephritis

Treatment :- Reduction of body level of sodium by diaetary sodium intake in food & by increasing excretion by
kidney by using diuretics.

2. Potassium balance

A) Hypokalaemia

Causes :-
 Dietic deficiency
 High sodium intake in the food
 Administration of insulin
 Diarrhoea, Vomiting

Treatment :- Oral replacement

B) Hyperkalaemia

Causes :-
 Decreased renal excretion
 Cellular shifts
 Diabetes mallitus

Treatment :-
 Removal of K+ by, Loop diuretics or Haemodialysis.
 Shifting K+ in to cells by, Sodium bicarbonate (4.8 to 9.6 mEq IV)

42 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


VACCINES

 A vaccine is a biological preparation that provides active acquired immunity to a particular disease.
 A vaccine typically contains an agent that resembles a disease-causing microorganism and is often made from
weakened or killed forms of the microbe, its toxins or one of its surface proteins.
 The agent stimulates the body's immune system to recognize the agent as a threat, destroy it, and keep a record
of it, so that the immune system can more easily recognize and destroy any of these microorganisms that it later
encounters.

Types

1. Inactivated :- Some vaccines contain inactivated, but previously active, micro-organisms that have been destroyed
with chemicals, heat, radiation, or antibiotics.
Ex :- influenza, cholera, bubonic plague, polio, hepatitis A, and rabies.

2. Attenuated :- Some vaccines contain live, attenuated microorganisms. Many of these are active viruses that have
been cultivated under conditions that disable their virulent properties, or that use closely related but less dangerous
organisms to produce a broad immune response.
Ex :- the viral diseases yellow fever, measles, rubella, and mumps, and the bacterial disease typhoid, BCG.

3. Toxoid :- Toxoid vaccines are made from inactivated toxic compounds that cause illness rather than the micro-
organism. Examples of toxoid-based vaccines include tetanus and diphtheria. Toxoid vaccines are known for their
efficacy. Not all toxoids are for micro-organisms.
ex. Crotalusatrox toxoid is used to vaccinate dogs against rattlesnake bites.

4. Subunit :- Protein subunit – rather than introducing an inactivated or attenuated micro-organism to an immune
system (which would constitute a "whole-agent" vaccine), a fragment of it can create an immune response.
Ex :- subunit vaccine against Hepatitis B virus that is composed of only the surface proteins of the virus.

5. Conjugate :- Certain bacteria have polysaccharide outer coats that are poorly immunogenic. By linking these outer
coats to proteins (e.g., toxins), the immune system can be led to recognize the polysaccharide as if it were a protein
antigen. Ex. Haemophilusinfluenzae type B vaccine.

SOME VACCINES

 BacilleCalmette-Guerin or BCG vaccination

 At birth or within six weeks of birth. (though the Indian Academy of pediatrics says it should be administered within two
weeks from birth).
 BCG is given over the left shoulder, in the form of an injection
 It protects the child against TB.
 After about a month a small swelling appears at the site of the injection, which can break into an ulcer with some liquid
discharge. Eventually the ulcer heals leaving a permanent scar. Do not try to treat the ulcer with any medication or
ointment.

 Oral Polio vaccination (OPV)

 At birth, 6th, 10th, 14th weeks and another dose between 16th to 18th month
 Oral polio is administered orally to the baby
 It saves baby from the crippling polio virus and its other consequences
 Since it is an oral vaccination make sure don’t feed baby 10 to 15 minutes prior to the dose to avoid vomiting.

43 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


 Diphtheria, Pertussis, tetanus vaccination (DPT)

 At 6th, 10th, 14th week, a booster shot is given between 16th to 18th month
 In an injection form where one dose is capable to defend baby against three diseases. Baby needs four doses of DPT to
be immunized against the three conditions.
 This vaccination protects baby from diphtheria, pertussis, tetanus failing to which it would prove to be fatal if your baby
suffers from any of these three infections.
 A little fever after this dose can be expected. Usually it lasts for 24 hours or little more than that.

 Measles Vaccination

 At 9th month
 The measles vaccine is administered subcutaneously, i.e. just below the skin.
 It protects baby from measles viral infection that can progress to cause diarrhea, pneumonia and in some cases even
prove fatal.
 It is mandatory to vaccinate the child with a measles vaccine.

 Hepatitis B vaccination

 At birth, between 6th to 14th week, 6th month


 For the three doses subsequent injections are given to the baby to complete the cycle.
 It is given to prevent jaundice caused by the Hepatitis B or serum hepatitis virus, which can be passed from an affected
mother to the baby or from one affected member of the family to another.
 It is a highly recommended vaccination.

 HIB Vaccination

 6th, 10th and 14th week and between 15th and 18th month
 In injection form four times to ensure baby’s safety.
 This vaccine provides protection against Haemophilus influenza type B that can result in childhood diseases of
pneumonia, bacterial meningitis and septicemia.
 Hib becomes an important vaccination for child because of the severity it can cause if you fail to give baby the doses on
time.

 MMR vaccination

 15th to 18th months


 One vaccination injection usually given on the thigh
 This vaccine confers immunity against measles, mumps and rubella or German measles.
 Might also advise a repeat dose of MMR at the age of 12 for added protection.

 Varicella

 Above 1 year
 It is given twice one after 12 months and the other when the child is between 4 to 6 years old.
 This is given to protect baby from the deadly chicken pox virus.
 Though an important vaccination but it is not mandatory. It still sounds wise to opt one for baby.

 Rotavirus

 4th and 6th month


 This is given orally to your baby at the doctor’s clinic.
 This vaccine is administered to provide immunity against rotavirus infection. The virus can cause severe gastroenteritis
along with diarrhea and vomiting that can seriously impact the health of your baby.

44 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


Adverse reaction

• Local tenderness, erythema, induration, fever, arthralgia and malise.


• Allergic reaction

Contra-indication

• Severe acute illness


• Pt. receiving immunosuppressive therapy or radiotherapy.
• Chik embryo culture vaccine in allergic to egg, chicken or chicken feathers.

Recommended immunization schedule followed in India (active immunity)

Sl No. Age Disease Vaccination


1 AT BIRTH HEPATITIS B HEP B VACCINE -I

2 AT BIRTH POLIO ORAL PV 0 DOSE

3 BIRTH TO 6 WK TUBERCULOSIS BCG

4 4 -6 WEEKS HEPATITIS B HEP B VACCINE -II

5 6 WEEKS DIPHTHERIA PERTUSIS TETANUS POLIO DPT-I OPV -I

6 10 WK DIPHTHERIA PERTUSIS TETANUS POLIO HEPATITIS B DPT-II OPV-II HEP B VACCINE III*

7 14 WEEKS DIPHTHERIA PERTUSIS TETANUS POLIO DPT-III OPV- III HEP B VACCINE IV*

8 24 WEEKS HEPATITIS B HEP B VACCINE III*

9 9 -12MTHS POLIO MEASLES OPV-IV MEASLES

10 15-18 MTHS MUMPS MEASELES RUBELLA MMR*

11 18 MTHS DIPHTHERIA PERTUSIS TETANUS POLIO DPT –BOOSTER I OPV –V

12 24 MTHS TYPHOID TYPHOID*

13 4-5 YR DIPHTHERIA PERTUSIS TETANUS, POLIO DPT BOOSTER – II OPV -VI

45 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


ANTI-SNAKE VENOM

 Anti-snake venom is obtained from immunized horses contain the purified antitoxin globulins that have the
power of neutrilising the venom of cobra, crait, russell’s viper and saw-scaled vipers.

 It is reconstituted by adding 10 ml of distilled water.

 A sensitivity test is performed by injecting 0.02-0.1 ml of 1:10 diluted antivenom SC. If no reaction occurs within
30 min., 20-40 ml injected IV, very slowly (0.5-1ml/min). Repeated dose is given if necessary, every 3-4 hours up
to a total of 100 ml. depending on severity of case.

 In case of viper bites some serum is injected around the bite to prevent development of gangrene.

ANTI-RABBIES

Rabies vaccine is used for prevention from rabies caused by bite or contact with dog, bat and other animals.
Many types of rabies vaccines are available in market as shown below,

Vaccine type Pre-exposure treatment Post exposure treatment


Sample vaccine
Given SC in to the cellular tissue on Given 2 ml SC on lower abdominal wall
(sterile suspension of sheep brain the side of the abdominal wall. daily for 14 days with booster doses on
substance containing fix virus of rabies) Immunity lasts only for 3 months. 21,28 and 91 days.

HDCV (Human Diploid Cell


inactivated Vaccine) 3 dose, 1 ml IM in deltoid on 0, 7 5 doses IM on 0, 3, 7, 14 and 28 days.
and 21 or 28 days
Obtained from human fibroblast culture

PCECV (Purified Chick Embryo


Cell rabies Vaccine)
Doses as above Doses as above
obtained by growing the virus in primary
cultures of chick fibroblasts. (RABIPUR)

PVRV -
(Purified Verocell Vaccine) 5 doses, 0.5 ml IM similar to HDCV

Rabies antiserum :-
 This is a hyper immune, horse serum containing the globulins that have specific power of neutrilising the rabies virus.
Usually given along with rabies vaccine in patients who have received severe bites.
 Dose: - not less than 400 units are infiltrated around the wounds and at the same time 40 units/kg is given IM.
 Adverse reactions :- Possibility of severe allergic reactions.

Rabies immune globulin (RIB) :-


 Prepared from plasma of donors hyper immunized with the rabies vaccine.
 It is indicated for known or suspected severe exposure to rabies virus
 Given in conjugation with rabies vaccine
 Dose is 20 IU/kg; one half dose should be infiltrated around the wound.

46 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


LOCAL ANTI-SEPTICS
Antiseptic is a chemical disinfectant (usually bacteriostatic) that can be diluted sufficiently to be safe for application
to living tissue while still retaining its antimicrobial property.

Not only medicine but used daily like sops, toothpaste, mouth wash, after shave etc.

Classification :-

A) Physical agents :- Heat, Filtration, Radiation


B) Chemical agents :-

1. Acids  Inorganic compound:- Boric acid


aqueous solution (2-4%) are used as mouth wash, eye and skin lotions.
 Organic compound:- Benzoic acid (ringworm infection),
Salicylic acid (seborrhoegic dermatitis, acne, fungal disease).

2. Alkalis  Sodium hydroxide


Used for disinfecting excreta from patients with  Potassium hydroxide.
Poliomyelitis
3. Alcohols  Ethanol :- skin antiseptic (70%), poor activity against bacterial spores
 Isopropyl alcohol :- more potent than ethyl alcohol, skin antiseptic

4. Aldehydes  Formaldehyde :- its 40% solution containing methanol (formalin) is highly


disinfective against bacteria, viruses and fungus. Used as common preservative and
as a disinfectant.

5. Surfactants  Anionic surfactants :- Soaps, sodium lauryl sulfate, sodium cetostearyl sulfate
(shampoo, skin cleanser)
 Catonic surfactants :- benzalkonium chloride, cetrimide (Savlon)

6. Phenols and related compounds  Cresol


 Lysol
oldest antiseptic, not used recently because of its  Chloroxylenol (Dettol) (1.44%): less toxic.
corrosive effect.  Thymol
 Savlon :- effective against wide range of gram positive and negative bacteria (5%)

7. Halogens and related compounds  Iodine :- most potent bacteriocidal agent and highly sporicidal, fungicidal,
amoebicidal and moderate viricidal
o Strong iodine tincture (10%)
o Weak iodine tincture (2%)
o Aqueous iodine solution (Lugol’s solution)
 Chlorine and chloramines :- commonly used for purification of water. Also used as
disinfectants.

8. Oxidizing agent  Hydrogen peroxide (H2O2) :- used for cleansing the wounds, abscess, for removing
of adhering dressing. Ear drops for removal of ear wax, used for deodorant gargle
or mouth wash.
 Potassium and Zinc permanganates :- used for gargles, mouth wash, vaginal
irrigation. Crystalline insufflations employed in snake bite and scorpion bite to
oxydise the venom. Used for stomach wash.

9. Heavy metals  Silver compound :-


o Silver nitrate and silver sulfadiazine:
o Used as antiseptics in eye drops (1%)
o Burns (0.5%)
 Zinc salts :-
o Zinc sulfate (eye drops)
o Calamine (sunburns, eczema, urticaria)
o Zinc phosphate (rat poison)

47 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


DRUGS IN OPHTHALMIC PRACTICE
In ophthalmic practice, local congestion, inflammation, allergy & glucoma require medical treatment. In addition
miotics, mydriatics, local anaesthetics & fluorescent dyes are used either for treatment, surgical procedure or for
diagnosis.

Classification :-

1. Anti-microbials (i) Anti-bacterial


 Ciprofloxacin
 Ofloxacin
 Gentamycin

(ii) Anti-fungal
 Fluconazole
 Miconazole

(iii) Anti- viral


 Acyclovir

2. Anti-inflammatory & Anti-allergic (i) Steroids


 Dexamethasone
 Betamethasone

(ii) NSAIDs
 Diclofenac
 Suprofen

(iii)Anti allergic
 Oloparadine
 Emedastine

(iv) Decongestants
 Nephazoline
 Phenylephrine

3. Drugs used in glaucoma (i) Cholinergic agents (increase outflow)


 Pilocarpine

(ii) α-Adrenergic agonists (increase outflow)


 Dipiverfrine

(iii) β-Adrenergic blockers (decrease secretion)


 Betazolol

(iv) Carbonic anhydrase inhibitors (decrease secretion)


 Dorzolamide

(v) Prostaglandins
 Latanoprost

48 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


4. Mydriatics & cycloplegics (i) Anti-cholinergics
 Atropine
 Homatopine

(ii) Adrenergics
 Phenylephrine

5. Topical anaesthetics  Benzocaine


 Dyclonine
 Lignocaine
 Tetracaine

6. Preservatives in ocular preparations  Banzalkonium


 Chlorbutanol
 Thiomersol

7. Miscellaneous (i) Diagnostic dye


 Fluorescein
 Rose bengal

(ii) Anti-cataract agents


 Glutathione
 Catalin

(iii) Anti-septic
 Povidone-iodine

49 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


ANTI-CANCER DRUGS
Pathology :-
In the cancer cells the cell cycle control is desturbed by

 Abnormal growth factor function


 Abnormal CDK function
 Abnormal DNA synthesis
 Abnormal decrease in negative regulatory forces due to mutation in tumor supressor gene.

Mainly 2 types
1. Carcinoma :- Ca. of epithelial tissue.
2. Sarcoma :- Ca. of non epithelial tissue.

Difference of cancer cells from healthy cells.


 Uncontrolled proliferation.
 Differentiation and loss of function.
 Invasiveness
 Metastasis

Classification :-

1. Alkylating agents • Mechlorethamine (Mustine)


• Cyclophosphamide (Endoxan)
• Mephalan (Alkeran)
• Thiotepa

2. Antimetabolites • Methotraxate (oral/IV)


• 6-mercaptopurine (oral)
• 5-fluorouracil (IV)
• Cytosine arabinoside

3. Radioactive isotopes • Radioiodine (Na131): given orally, useful in thyroid ca.


• Radioactive gold (198AU): useful in malignant pleural
and peritoneal effusions.

4. Cytotoxic antibodies • Actinomycin D


• Doxorubicin
• Bleomycin
• Mytomycin C

5. Antimitotic plant products • Paclitaxel: derived from western yew tree.


• Camptothecin analogues: derived from Camptotheca
acuminata.
• Etoposide: derived from Podophyllum peltatum

6. Hormones & antihormones • Estrogens: prostatic cancer


• Progestins: endometrial ca.
• LH-RH antagonist: metastatic ca in prostate.

7. Biological response modifires • Immunostimulants such as BCG, levamisole etc.

8. Monoclonal antibodies & tyrosine kinase inhibitors • Trastuzumab


• Bevacizumab

50 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17


IMMUNO-MODULATORS

Agents that alter the immune response by suppression (immuno-suppressive) or enhancement (immuno-stimulant).

Classification :-

1. Immuno-suppresers (i) Glucocorticoids

Glucocorticoids are used to suppress various allergic, inflammatory, and auto


immune disorders. They are also administered as post transplantory
immunosuppressants to prevent the acute transplant rejection and graft-versus-
host disease. Nevertheless, they do not prevent an infection and also inhibit later
reparative processes.
Compounds and dose:-
Prednisolone: 10-100 mg daily in divided dose; 25 mg IM
Pediatric: drops 5 mg/ml
new born: 0.3-0.4 mg/kg
older: 0.15-0.2 mg/kg

(ii) Calcineurine inhibitors

Compounds :-
• Cyclosporine: oral (capsule and solution)/IV
• Tacrolimus: oral/IV

(iii) Cytotoxic/ antiproliferative agents

Cytostatics (cytotoxic) inhibit cell division. In immunotherapy, they are used in


smaller doses than in the treatment of malignant diseases. They affect the
proliferation of both T cells and B cells.
Compounds :-
• Azathioprine
• Methotrexate

(iv) Antibodies
• Muronomab
• Antilymphocytic antibodies
• Basiliximab
• Daclizumab

2. Immuno-stimulants (i) Specific immunostimulants provide antigenic specificity in immune response,


such as vaccines or any antigen.
(ii) Non-specific immunostimulants non-specific immunostimulants do not have
any antigenic specificity but can act as general stimulants that enhance the
function of certain types of immune cells.

Compounds :-
• Thalidomide
• Levamisole
• Glatiramer acetate

51 Alpesh B. Munjani J.S. Ayurveda Mahavidhyalaya, Nadiad. Oct-17

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