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The document discusses several drug combinations used to treat different conditions. It provides details on the individual drugs in each combination, their mechanisms of action, synergistic effects, uses, doses and adverse effects.

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Ankit Pandey
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10 views

FDC

The document discusses several drug combinations used to treat different conditions. It provides details on the individual drugs in each combination, their mechanisms of action, synergistic effects, uses, doses and adverse effects.

Uploaded by

Ankit Pandey
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Download as PDF, TXT or read online on Scribd
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1.

IMIPENEM+CILASTIN
Imipenem is an extremely potent broad spectrum antibiotic
with a range including gram+ve cocci,enterobactriacese,
neisseria,anaerobes, clostridium. Resistant to most Beta
lactamases, inhibits penicillinase producing staphylococci and
some MRSA.
Cilastin is a reversible inhibitor of dihydropeptidase it has same
pharmacokinetics as imipenem half life of one hour protects it
Imipenem +Celastin 0.5 g, IV. 6hourly with maximum of 4 gm
/day
Noscomial Infection
At this dose it is effective in wide range of hospital acquired
infections including those with neutropenia and cancer patient
and also Aids patients.
SE Nausea Diaroha Rashes zianes

2. DIPHENOXYLATE+ATROPINE.
It is used as antidiarrhoeal drug. Diphenoxylate (2.5mg) +
Atropine(0.025mg) Dose 5-10 mg followed by 2.5 mg- 5mg / 6
hours
Diphenoxylate is an antimotility drug. It is synthetic opioid
chemically related to pethidine used exclusively as a
constipating agent.
They reduce propulsive movement and diminish Intestinal
motility & enhance absorption of intestinal soluble contents.
The major action appears to be mediated through MEU opioid
receptors located on enteric neuronal network.MEU receptor
is a G-p rotein coupled receptor which prevents opening of
calcium channel in presynaptic region &opens the calcium
channel in postsynaptic region leading to spasm of intestinal
smooth muscle. So there is constipating action due to spasm of
the intestinal smooth muscle & decreased intestinal motility. It
crosses blood brain barrier & produces CNS effects. Higher dose
on prolonged use can produce opioid dependence. If atropine
(0.025mg) is added to 2.5mg of diphenoxylate this opioid
dependence can be prevented because atropine also produces
constipating action & decreases the dose of diphenoxylate
required to produce anti motility action. At this lower dose
diphenoxylate does not produce dependence.
Atropine is an anticholinergic drug. It relaxes visceral smooth
muscle by causing M3 receptor blockade & inhibiting action of
Acetyl choline. Tone and amplitude of contraction of smooth
muscle in intestine is reduced. Passage of chyme is slowed.
Constipation may occur, spasm may be relieved. Overdose will
produce disturbing atropinic side effects like respiratory
depression, paralytic ileus and toxic megacolon in children. It is
contraindicated in very young children.
4.COTRIMOXAZOLE

It is fixed doe combination of


Trimethoprim+Sulfamethoxazole.

Trimethoprim: It is a dopaminergic agent. It selectively


inhibits bacterial dihydrofolate reductase. Therefore
human folate metabolism is not interfered with at
antibacterial concentration of Trimethoprim. It is
bacteriostatic and enters many lesions, attains larger
volumes of distribution than Sulfamethoxazole. It crosses
Blood Brain Barrier and placenta. It is bound to plasma
proteins and metabolized in liver.

Sulfamethoxazole: It is selected in this combination,


because both have same halflives. It inhibits folate
synthetase. The combination is highly effective because
these drugs act as bactericidal in this combination but they
act as bacteriostatic individually. Maximum synergism is
seen when used against bacteria susceptible to both
drugs.
1. If bacteria is resistant to any one drug the action of the
other drug is enhanced.
2. The ratio of 5:1(S: T) have maximum synergism.
3. Antibacterial spectra of both drugs overlapped considerably.
4. Resistance to the combination develops slowly compare to
the individual drugs.
Adverse effects
1. Nausea, vomiting, diarrhorea, headache, rashes, blood
disorders.
2. All adverse effects seen with sulfonamides can be
produced in the combination
3. It should not be given during pregnancy because
trimethoprim causes neonatal haeomolysis and
methhaemoglobinemia.
4. It causes uraemia in patients with renal disease.
5. High incidence of fever with rashes and bone marrow
depression due to cotrimaxazole is seen in aids patients
with pneumocystis infection.
6. Diuretics with cotrimaxazole cause thrombocytopenia.

USES
1. Urinary tract infections
2. Upper and lower respiratory tract infections
3. Bacterial diarrhorea and dysentery
4. Typhoid fever
5. Chancroid
Dose: Sulfamethamaxazole 400mg +Trimethoprim 80mg

1. LEVODOPA+ CARBIDOPA
It is used in the treatment of Parkinson’s disease. L-
dopa is inactive by itself but is an immediate
precursor of dopamine. More than 95% of oral dose
is decarboxylated in the gut and liver by DOPA
decarboxylase. Dopamine acts on heart blood vessels
peripheral organs and CTZ.
About 1-2% of administered L-dopa crosses blood brain
barrier and taken up by dopaminergic neurons and
converted into dopamine which is stored in the neurons.

Carbidopa is inhibitor of DOPA decarboxylase in the extra


cerebral tissues. It does not penetrate blood brain barrier.
When administered along with L-dopa it inhibits DOPA
decarbaxylase and increases plasma t ½ L-dopa in the
periphery and makes it available to cross blood brain
barrier.
Advantages
1. Plasma t ½ of L-dopa is prolonged and the dose of L
dopa is reduced to ¼ th of original dose.
2. Systemic concentration of dopamine is reduced.
Therefore side effects like nausea and vomiting are not
NOT SEEN
prominent. Therapeutic dose of L-dopa can be attained
quickly.
3. Cardiac complications are minimized.
4. Pyridoxine reversal of L-dopa does not occur.
5. ON and OFF effects are minimized since the cerebral
concentration of dopamine is sustained .So the patients
who are not responding to levodopa alone can improve
when given in combination with carbidopa.
This combination is called co- carbidopa .
Disadvantages
The following problems are not resolved by the combination
1. Involuntary movements
2. Behavioural abnormalities
3. Postural hypo tension
Currently L-dopa is always used with decarbaxylase inhibitors
except in those patients who develop marked involuntary
movements.

6. PYRIMETHAPRIM+SULFADOXINE
Pyrimethaprim is a diamminopyridine derivative. It
selectively inhibits dihydrofolate reductase and
interferes with synthesis of folic acid in the parasite. It
is slow acting erythrocytic schiznticidal agent . If is used
alone develops rapid resistance by mutation of
dihydrofolate reductase enzyme in malarial parasite.
The drug is metabolized in liver and excreated in kidney.

Sulfadoxine It is long acting sulfonamide which


compitetively inhibits folates synthase enzyme. It is
effective against a sexual form of the parasite. The
combination is effective due to sequential blockade in
prossstozoan folic acid synthesis. There is least chance
of developing resistance but the combination acts
faster.

Uses Clinically used in


1. Treatment of falciparum malaria
2. As an adjuvant drug with quinidine in treatment of
chloroquine resistant falciparum malaria
3. Prophylaxis for travelers who go to falciparum
malaria endemic areas
4. 1st line therapy for treatment of toxoplasmosis in
immune compromised patients
5. Folic acid is usually co administered to limit bone
marrow suppression
Adverse effects
1. Megaloblastic anemia
2. Granulocytopenia
3. Atrophic glossitis
4. Steven’s Johnson’s syndrome
5. Allergic alveolitis

Dose: Sulfadoxine 500mg + pyrimethamine 25mg or


Sulfadoxine 700mg+pyrimethamine 37.5 mg

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