Drug profiles of Vancomycin, Prednisone and Salbutamol

VANCOMYCIN
VANCOMYCIN HYDROCHLORIDE
By: Komal Haleem, Pharm-D

•Vancomycin is a glycopeptide antibiotic used
in the prophylaxis and treatment of infections
caused by Gram-positive bacteria.
•Vancomycin is used to treat infections of the
intestines that cause colitis (inflammation of
the large intestine).
DESCRIPTION

BRAND NAMES
VANCOCIN
ELI LILLY PAKISTAN (PVT)
LTD.
VANCOMYCIN
ABBOTT
LABORATORIES
(PAKISTAN) LIMITED.

PREPARATIONS
 125 mg
 250mg
 500 mg
 750mg
 1g
 5g
 10g
- Capsules, oral
- Injection, lyophilized powder for solution:
- Injection, frozen, premixed solution:
 500 mg per 100 mL
 750 mg per 150 mL
 1 g per 200 mL

INDICATIONS AND USAGE
ORAL
• Treatment of Clostridium difficile –associated diarrhea
• Treatment of staphylococcal enterocolitis.
PARENTERAL
• Treatment of serious or severe infections caused by
susceptible strains of methicillin-resistant
(beta-lactam–resistant) staphylococci
• Treatment of staphylococcal, streptococcal, enterococcal,
or diphtheroid endocarditis.

UNLABELLED USES
Aerosolization
Central venous catheter infection
 Preoperative prophylaxis
 Rectal administration
 Ventricular shunt infections.

Inhibits cell wall synthesis.
Inhibits transglycosylase.
Alters cell membrane permeability.
Cell becomes susceptible to lysis.
MECHANISM OF ACTION

ABSORPTION
 Poorly absorbed (orally).
 When given by injection:
• C max is 63 mcg/mL
• T max is 1 h (injection)

DISTRIBUTION
 55% protein bound.
 Vd is 0.3 to 0.43 L/kg.
 Distributes in:
• Pleural fluid
• Pericardial fluid
• Ascitic fluid
• Synovial fluid
• Urine
• Peritoneal dialysis fluid
• Atrial appendage tissue

No apparent metabolism of the drug.

 IV: about 75% is excreted in the urine by
glomerular filtration (in the first 24 hrs).
 Mean half-life is 4 to 6 hrs.
 Oral: feces

SPECIAL POPULATIONS
RENAL FUNCTION IMPAIREMENT:
 Slows excretion of vancomycin
 In anephric patients: half-life is 7.5 days.
 Dosage adjustment is required.
ELDERLY:
 Total systemic and renal Cl may be reduced.
 Dosage adjustment is required.

Endocarditis (staphylococcal, streptococcal,
enterococcal, diphtheroid), staphylococcal
infections
IV 500 mg every 6 h or
1 g every 12 h at a rate
no faster than 10
mg/min or over at least
60 min, whichever is
longer.
IV 10 mg/kg per
dose given every 6
h over at least 60
min.
IV initial dose of 15
mg/kg, followed by 10
mg/kg every 12 h in the
first week of life and
every 8 h thereafter up
to 1 month of age.

C. difficile –associated diarrhea
PO 125 mg 4 times daily for
10 days.
PO 40 mg/kg/day in 3 or 4
divided doses for 7 to 10
days; max dosage is 2 g/day.

Staphylococcal enterocolitis
PO 500 mg to 2 g in 3 or 4
days.
PO 40 mg/kg/day in 3 or 4
days

 Cardiovascular
Hypotension.
 CNS
Headache, fatigue, dizziness, vertigo (rare).
 Dermatologic
Drug rash, exfoliative dermatitis, pruritus, Stevens-
Johnson syndrome, urticaria, vasculitis.
 Hematologic
Reversible agranulocytosis; eosinophilia,
thrombocytopenia
 ENT
Hearing loss; tinnitus (rare).

 GI
Nausea; abdominal pain; diarrhea, vomiting; flatulence;
antibiotic-associated colitis.
 Genitourinary
UTI; nephrotoxicity including increased blood creatinine,
renal failure, and renal impairment
 Local
Injection-site inflammation.
 Respiratory
Dyspnea, wheezing.
 Red man syndrome
Flushing of the face, neck, upper chest,
and extremities
 Hypokalemia
 Pyrexia

PRECAUTIONS
 Pregnancy
Category C (injection); Category B (oral).
 Lactation
Excreted in breast milk.
 Renal Function
Dosage adjustments required; use with caution.
 Children
Confirming serum levels is recommended.
 Elderly
Adjust dosage schedules.
 Administration
Give by secure IV route. May minimize thrombophlebitis by
giving slowly as dilute infusion.

CONTRAINDICATIONS
 Hypersensitivity to vancomycin
 Hypersensitivity to corn
or corn products.

OVERDOSAGE
 Hearing loss,
 increased BUN,
 increased serum creatinine,
 ringing in ears,
 vertigo.

DRUG INTERACTIONS
ANESTHETICS
• increased risk of hypersensitivity &
infusion-related reactions
INDOMETHACIN • increases vancomycin toxicity in neonates.
METHOTREXATE
• increases methotrexate toxicity
NON DEPOLARIZING
MUSCLE RELAXANTS
• neuromuscular blockade may be enhanced
AMINOGLYCOSIDES,
AMPHOTERICIN B,
BACITRACIN, CISPLATIN,
POLYMIXIN B
• increases risk of nephrotoxicity and/or
neurotoxicity.

Storage & Stability
Parenteral
 Store vials at 68° to 77°F.
 After reconstitution,
vials may be stored in a
refrigerator for 14 days.
Oral
 Store at 59° to 86°F.

PATIENT COUNSELING
 Explain that IV medication is given at regular intervals
to maintain blood levels.
 Tell patients to report hearing loss, ringing in ears, or
vertigo to their health care provider.
 Identify symptoms of potential
adverse reactions.
 Tell patients to maintain adequate
fluid intake.
 Tell patients not to stop taking
vancomycin, even if they start to
feel better.

Prednisone is a corticosteroid. It prevents the release
of substances in the body that cause inflammation.
Prednisone also suppresses the immune system.
Prednisone is used as an anti-inflammatory or an
immunosuppressant medication
DESCRIPTION

BRAND NAMES
Prednisone Tablet
Watson Laboratories, Inc.
FORTIPRED
REMINGTON
PHARMACEUTICAL
INDUSTRIES (PVT) LTD.

INDICATIONS AND USAGE
1. Endocrine disorders;
2. rheumatic disorders;
3. collagen diseases;
4. dermatologic diseases;
5. allergic and inflammatory ophthalmic processes;
6. respiratory diseases;
7. hematologic disorders;
8. neoplastic diseases;
9. edematous states (because of nephrotic syndrome);
10. GI diseases;
11. tuberculous meningitis;
12. trichinosis with neurologic or myocardial involvement.

UNLABELLED USES
 COPD;
 Duchenne muscular dystrophy;
 Graves ophthalmopathy.

PHARMACOLOGY
Intermediate-acting glucocorticoid
that depresses formation, release, and
activity of endogenous mediators of
inflammation, including
prostaglandins, kinins, histamine,
liposomal enzymes, and complement
system.
Also modifies body's immune
response.

 Absorption
Rapid, almost complete.
 Distribution
Crosses placenta.
 Metabolism
Mainly hepatic, also renal and in the tissue. Prednisone
is inactive and rapidly metabolized to active
prednisolone.
 Elimination
Renal. Plasma t ½ is 3.4 to 3.8 h.
 Peak
1 to 2 h.
 Duration
1.25 to 1.5 days.

 Adults
PO 5 to 60 mg/day.
 COPD Adults
PO 30 to 60 mg/day for 1 to 2 wk, then taper.
 Duchenne Muscular Dystrophy Adults
PO 0.75 to 1.5 mg/kg/day.
 Graves Ophthalmopathy Adults
PO 60 mg/day; taper to 20 mg/day.

CONTRAINDICATIONS
 Systemic fungal infections
 administration of
live virus vaccines.

DRUG INTERACTIONS
 Anticholinesterases
Antagonizes anticholinesterase effects in myasthenia
gravis.
 Anticoagulants, oral
Alters anticoagulant dose requirements.
 Barbiturates, hydantoins (eg, phenytoin),
rifampin
Decreased pharmacologic effect of prednisone.
 Cyclosporine
Enhanced cyclosporine toxicity.

 Estrogens, ketoconazole,
oral contraceptives
Decreased Cl of prednisone.
 Nondepolarizing muscle relaxants
May potentiate, counteract, or have no effect on
neuromuscular blocking action.
 Salicylates
Reduced serum levels and efficacy of salicylates.
 Somatrem
Inhibition of growth-promoting effects of somatrem.
 Theophylline
Alterations in pharmacologic activity of either agent.

 Cardiovascular
Thromboembolism or fat embolism; thrombophlebitis; cardiac
arrhythmias or ECG changes; hypertension; myocardial rupture;
CHF.
 CNS
Convulsions; pseudotumor cerebri; vertigo; headache;
psychosis.
 Dermatologic
Impaired wound healing; thin fragile skin; erythema; lupus
erythematosus-like lesions; subcutaneous fat atrophy; purpura;
hirsutism; acneiform eruptions; allergic dermatitis; urticaria;
angioneurotic edema
 EENT
Posterior subcapsular cataracts; increased IOP; glaucoma;
exophthalmos.

 Genitourinary
Increased or decreased motility and number of
spermatozoa.
 Hematologic
Leukocytosis.
 Metabolic
Sodium and fluid retention; hypokalemia; hypokalemic
alkalosis; metabolic alkalosis; hypocalcemia.
 GI
Pancreatitis; abdominal distention; ulcerative
esophagitis; nausea; vomiting; increased appetite and
weight gain; peptic ulcer with perforation and
hemorrhage; small and large bowel perforation.

PRECAUTIONS
 Pregnancy
Category C .
 Lactation
 Children
 Elderly
 Renal Function
 Hypersensitivity

 Adrenal suppression
 Cardiovascular effects
 Hepatitis
 Immunosuppression
 Infections
 Ocular effects
 Use systemic drug cautiously in ocular herpes simplex
because of possible corneal perforation.
 Ophthalmic use
 Peptic ulcer
 Stress
 Withdrawal
Abrupt discontinuation may result in adrenal insufficiency.

OVERDOSAGE
 Cushingoid changes, Moonfaced, central obesity
 hirsutism, acne, ecchymoses, hypertension,
 osteoporosis, myopathy
 sexual dysfunction
 diabetes mellitus, hyperlipidemia
 peptic ulcer, GI bleeding
 increased susceptibility to infection
 electrolyte and fluid imbalance
 psychosis

DESCRIPTION
 Salbutamol tablets belong to a group of medicines called
selective beta-2-adrenergic agonists, which can be used to
relax the muscles of the airways.
 Salbutamol is available for administration by the following
routes:Inhalation, tablet, elixir, intravenous injection,
subcutaneous injection,intramuscular injection

INDICATIONS
 Salbutamol is a beta-adrenergic stimulant which has a highly
selective action on beta2-receptors in bronchial smooth muscle
and in therapeutic dosage, little or no action on cardiac beta1-
receptors.
 Salbutamol has an advantage in asthma treatment by
minimising side effects associated β1 receptor stimulation

•Asthma, to relieve the narrowing of the airways
•Chronic bronchitis
•Emphysema
•Prevention of premature labour.
USAGE

DISTRIBUTION
 Salbutamol binds to and releases from plasma
proteins as necessary.

METABOLISM
Salbutamol absorbed in the gastrointestinal tract
has a substantial ﬁrst pass metabolism and is
metabolized into Phenolic Sulfate.
 Inhaled Salbutamol acts directly on smooth
muscle of the upper airways bypassing
metabolism in the liver.

EXCRETION
 Excretion
 Salbutamol and Phenolic Sulfate are primarily
excreted via the urinary system.

DOSAGE AND ADMINISTRATION
 Ventolin S.R. Tablets must be swallowed whole with a glass of
water and not chewed or crushed.
 Adults:
Usual dose is 4mg three or four times a day. Your doctor may
increase this gradually up to a maximum of 8mg three or four
times a day. Some patients may be treated successfully with
2mg three or four times a day.

 Children 2-6 years:
1-2mg three or four times a day.
 Children 6-12 years:
2mg three or four times a day.
 Children over 12 years:
2-4mg three or four times a day.
 Children under 2 years:
Not recommended.
 Premature labour:
The maintenance dose is 4mg three or four times a day.
DOSAGE AND ADMINISTRATION

CONTRA-INDICATIONS
 Ventolin oral preparations are contra-indicated in patients with
a history of hypersensitivity to any of their components.
 Intravenous salbutamol and occasionally salbutamol tablets are
used in the management of premature labour uncomplicated by
conditions such as placenta praevia, antepartum heamorrhage
or toxaemia of pregnancy.
 Salbutamol presentation should not be used for threatened
abortion.

WARNINGS
 Increase use of short-acting inhaled beta2-agonists to control
symptoms indicates deterioration of asthma control.
 Sudden and progressive deterioration in asthma control is
potentially life-threatening and consideration should be given
to starting or increasing corticosteroid therapy.
 If dose fails to give usual relief, medical advice should be
sought.

PRECAUTIONS
 Salbutamol and non-selective beta-blocking drugs, such as
propranolol, should not usually be prescribed together.
 Salbutamol should be administrated cautiously to the patients
suffering from thyrotoxicosis.
 Particular caution is advised in acute severe asthma, as this
effect may be potentiated by concomitant treatment with
xanthine derivatives, steroids, diuretics and by hypoxia.

Administration of drugs during pregnancy should
only be considered if the expected benefit to the
mother is greater than any possible risk to the fetus.
PREGNANCY

Salbutamol is probably secreted in breast milk, its
use in nursing mothers is not recommended unless
the expected benefits outweigh any potential risk. It
is not known whether salbutamol in breast milk has
a harmful effect on the neonate.
LACTATION

SIDE EFFECTS
 Ventolin oral preparations may cause a fine tremor of
skeletal muscle in some patients.
 Occasionally headaches.
 Feeling of tension in some patients.
 Hypersensitivity reactions including angioedema,
urticaria, bronchospasm, hypotension and collapse have
been reported very rarely.

 An allergic reaction (hypersensitivity): swelling of the face, lips,
throat or tongue, pale or red irregular raised patches with severe
itching (hives), difficulty breathing, low blood pressure, collapse.
 Increased lactic acid in the body: rapid breathing, being sick,
stomach pain.
 Low blood potassium: muscle twitching or weakness, an irregular
heart beat.
SIDE EFFECTS

Salbutamol is not contra-indicated in patients
under treatment with monoamine oxidase
inhibitors ( MAOIs).
DRUG INTERACTIONS

Drug profiles of Vancomycin, Prednisone and Salbutamol

OVER DOSAGE
Antidote for over dosage with salbutamol is a
cardio-selective beta blocking agent.

•Storage :
Below 30˚C
•Don’t remove from
pack until required.
PHARMACEUTICAL
PRECAUTIONS

Drug profiles of Vancomycin, Prednisone and Salbutamol

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Drug profiles of Vancomycin, Prednisone and Salbutamol

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