Thursday, March 27, 2014
Cefuroxime
Indication
Cefuroxime is indicated in the treatment of
1. Upper respiratory tract
infections: For example, ear, nose and throat infections such as otitis media,
sinusitis, tonsillitis and pharyngitis.
2. Lower respiratory tract
infections: For example, acute bronchitis, acute exacerbations of chronic bronchitis
and pneumonia.
3. Skin and sft tissue
infections: Such as furunculosis, pyoderma and impetigo.
4. Genilo-urinary tract
infections: Such as pyelonephritis, urethritis and cystitis.
5. Gonorrhoea: Acute
uncomplicated gonococcal urethritis and cervicitis.
6. Early lyme disease and
subsequent prevention of late Lyme disease.
Pharmacology
Cefuroxime is a well-characterized and effective antibacterial
agent, which has broad-spectrum bactericidal activity against a wide range of common
pathogens, including β-lactamase producing strains. Cefuroxime has good stability
to bacterial β-lactamase and consequently, is active against many
ampicillin-resistant and amoxycillin-resistant strains.
Composition
Cefuroxime 125 mg tablet: Each film coated tablet
contains Cefuroxime 125 mg as Cefuroxime axetil BP.
Cefuroxime 250 mg tablet: Each film coated tablet
contains Cefuroxime 250 mg as Cefuroxime axetil BP.
Cefuroxime 500 mg tablet: Each film coated tablet
contains Cefuroxime 500 mg as Cefuroxime axetil BP.
Cefuroxime powder for suspension (70 ml): Each 5 ml
reconstituted suspension contains 125 mg Cefuroxime, as Cefuroxime axetil BP.
Cefuroxime 750 mg IM/IV injection: Each vial contains Cefuroxime
750 mg, as Cefuroxime sodium BP.
Cefuroxime 1.5 gm IV injection: Each vial contains
Cefuroxime 1.5 gm, as Cefuroxime sodium BP.
Dosage and Administration
Adults: Most
infections well respond to 250 mg b.i.d. In mild to moderate lower respiratory tract
infections e.g bronchitis 250 mg b.i.d. should be given. For more severe lower
respiratory tract infections or if pneumonia is suspected then 500 mg b.i.d.
should be given.
For urinary tract infections
a dose of 125 mg b.i.d. is usually adequate, in pyelonephritis the recommended dose
is 250 mg b.i.d. A single dose of one gram is recommended for the treatment of uncomplicated
gonorrhea.
Lyme disease in adults and
children over the age of 12 years: The recommended dose is 500 mg b.i.d. for 20
days.
Children:
The usual dose is 125 mg b.i.d. or 10 mg/kg b.i.d. to a maximum of 250 mg
daily.
For otitis media, in
children less than two years of age the usual dosage is 125 mg b.i.d. or 10
mg/kg b.i.d. to a maximum of 250 mg daily and in children over two years of age
250 mg b.i.d. or 15 mg/kg b.i.d. to a maximum of 500 mg daily.
There is no experience in
children under three months of age. The usual course of therapy in seven days. Cefuroxime
should be taken after food for optimum absorption.
Parental Dosage
Adults: Cefuroxime
750 mg to 1.5 g IM or IV every 8 hourly, usually 50 to 10 days.
Preoperative
prophylaxis: For clean contaminated or potentially contaminated surgical procedures,
administer 1.5 g IV prior to surgery ( half to one hour before ). Thereafter,
give 750 mg iV or IM every 8 hours when the procedure is prolonged.
Infants
and Children (>3 months): 50 to100 mg/kg/day in
equally divided doses every 6 to 8 hours. Use 100 mg/kg/day (not to exceed the
maximum adult dose) for more severe or serious infections.
Bone
and Joint Infections: 150 mg/kg/day (not to exceed the maximum
adult dose) in equally divided doses every 8 hours.
Bacterial
meningitis: Initially 200 to 240 mg/kg/day IV in divided
doses every 8 hours.
Direction for Reconstitution
Cefuroxime 750 mg intramuscular Injection: Add 3 ml water
for injection BP and shake gently for dispersion
For 750 mg intravenous
injection: Add 6 ml water for injection BP and shake gently for dispersion.
For 1.5 mg intravenous
injection: Add 16 ml water for injection BP and shake gently for dispersion.
For Suspension: shake the
bottle well before adding water. Then add 35 ml of boiled and cooled water
(with the help of the provided cup from different company) to the bottle. Then
continue shaking the bottle until the powder is dissolved property.
Contraindication
Cefuroxime is
contraindicated in patients with known allergy to Cephalosporins.
Side Effect
Cefuroxime has been
associated with nausea and vomiting in a small number of patients.
Acute Over dosage
Excessively large dosage of
all cephalosporins can cause cerebral irritation and may cause convulsions.
This complication is unlikely to occur in routine practice unless the patient
is in renal failure hemodialysis or peritoneal dialysis can remove Cefuroxime.
Precaution
As with antibiotics,
prolonged use of Cefuroxime may result in the over growth of non-susceptible organisms
(e.g. Canada enterococci, Clostridium difficult), which may require
interruption of treatment.
Use in Pregnancy and Lactation
While all antibiotics should
be avoided in the first trimester if possible. Cefuroxime has been safety used
in later pregnancy to treat urinary and other infections. The placental
transfer of Cefuroxime into the fetus was studied in 20 women and
therapeutically active concentrations were found in the serum of infants for up
to 6 hours after delivery. Cefuroxime is excreted in human milk and
consequently caution should be exercised when Cefuroxime is administered to a
nursing mother.
Drug Interaction
No potentially hazardous
interactions have been reported.
Storage Condition
Tablet:
Store below 30 degree C, protected from light and moisture.
Suspension:
Store below 25 degree C, protected from light and moisture.
Injection:
Store below 25 degree C, protected from light and moisture. Use reconstituted
solution immediately. The reconstituted solution is stable for 2 hours at room
temperature and for 12 hours when refrigerated at 2 degree to 8 degree Celsius.
How Supplied from different companies
Cefuroxime 125 mg tablet: Box containing 20 tablets in blister pack.
Cefuroxime 250 mg tablet: Box containing 20 tablets in blister pack.
Cefuroxime 500 mg tablet: Box containing 20 tablets in blister pack.
Cefuroxime powder for suspension (70 ml): Bottle containing 70 ml suspension (after
reconstitution).
Cefuroxime 750 mg IM/IV injection: Pack of 1 vial containing Cefuroxime 750 mg as
Cefuroxime sodium BP accompanied by a solvent ampoule of 10 ml water for
injection. It also contains a complementary pouch comprised of disposable
syringe (10 ml) needle, alcohol pad and first aid bandage.
Friday, March 21, 2014
Bromazepam
Description
:
Bromazepam
is a global anxiolytic with smooth and supprior efficacy. It is one of the
benzodiazepines having no side-effects like other benzodiazepines. It
effectively manages anxiety and also removes anxiety related various physiological
problems.
Mode of
action:
Bromazepam
binds with the specific site on the GABA receptor/chloride channel complex and
potentiates the effect of GABA, an important inhibitory transmitter in the CNS
which acts by opening chloride ion channels into cells.
Pharmacokinetics:
Peak plasma
concentration of Bromazepam is achieved within two hours after oral
administration. The absolute bioavailability of the unchanged substance is 60%.
On an average 70% of Bromazepam is metabolized in the liver. Bromazepam has an
elimination half-life around 20 hours, but the half-life may be longer in
elderly subjects. The metabolites are excreted in the urine mainly in
conjugated form.
Composition:
Bromazepam
tablet: Each tablet contains Bromazepam BP 3 mg
Indications:
Emotional
disturbances: Anxiety and tension states, as adjuvant therapy for anxiety in
depressed patients, nervous, tension, restlessness, anxiety and tension related
insommia. As an adjuvant to the treatment of an underlying disease responsible
for functional or psychosomatic impairments of various organs caused or
exacerbated by anxiety and tension.
Cardiovascular
and respiratory systems: Pseudo angina pectoris, precordial anxiety, tachycardia,
emotiogenic hypertension, dyspnea and hyperventilation; Gastrointestinal tract:
irrible bowel syndrome, ulcerative colitis, epigastric pain, spasm, meteorism
and diarrhea.
Urogential
tract: Irritable bladder, urinary frequency, dysmenorrhoea; Other psychosomatic
disturbances: Psychogenic headache, psychogenic dermatoses.
Bromazepam
is also suitable for treatment of
anxiety and tension states due to chronic organic diseases and as an adjuvant
to psychotherapy in psychoneuroses, acute alcohol withdrawal, adjunct for the
relief of muscle spasm.
Dosage and
Administration :
1.50mg to 12
mg three times daily according to condition or patient response and side-effect profile.
Average
outpatient dosage: 1.5 mg to 3 mg three times daily.
Severe
cases: 6 mg to 12 mg two to three times daily.
Contraindications:
Bromazepam
should not be used in case of hypersensitivity of benzodiazepines, respiratory depression,
severe hepatic impairment, myasthenia gravis and infant.
Side
Effects:
Drowsiness,
lightheadedness in the next day; confusion, ataxia and ammesia may occur.
Use in
pregnancy and lactation:
The
administration of Bromazepam is rarely justified in woman of childbearing potential.
Bromazepam should be avoided during
breast-feeding.
Precautions:
Bromazepam
should be used cautiously in respiratory diseases, muscle weakness and history
of alcohol or drug abuse.
Drug
Interactions:
Phenothiazines,
barbiturates, MAO inhibitors and psychoactive drugs may potentiate the action of
Bromazepam and should not usually be given concurrently.
Overdosage:
Manifestations
of overdoage include somnolence, confusion and respiratory and cardiovascular depression
with coma in severe cases.
Storage:
Store in a
cool and dry place, protected from light and children’s.
Ciprofloxacin
Ciprofloxacin : Which is a synthetic anti-infective agent. Ciprofloxacin
Has broad spectrum of activity. It is active against most
gram-negative aerobic bacteria including enterobacteriaceae and pseudomonas
aeruginosa. Ciprofloxacin is also active against gram-positive aerobic bacteria
including penicilinase producing and methicilin resistant staphylococci,
although many strains of streptococci are relatively resistant to the drug. The
bactericidal action of Ciprofloxacin results from interference with the enzyme
DNA gyrase needed for the synthesis of bacterial DNA. Following oral
administration it is rapidly and well absorbed from the G.I tract. It is widely
distributed into body tissues and fluids. The half-life is about 3.5 hours.
About 30% to 50% of an oral dose of Ciprofloxacin is excreted in the urine
within 24 hours as unchanged drug and biologically active metabolites.
Indication: Ciprofloxacin is used adults for the treatment of
urinary tract infections, lower respiratory tract infections, shin and soft
tissue infections, bone and joint infections and G.I infections, caused by
susceptible gram-negative and gram-positive aerobic bacteria. It is also used
for the treatment of uncomplicated gonorrhea caused by penicillinase producing
neisseria gonorrhea. Ciprofloxacin 750 tablet is specially indicated for the
treatment of pseudomonal infections of lower respiratory tract, severe
infections particularly due to pseudomonas, staphylococcus and streptococci.
Ciprofloxacin 750 is also indicated in surgical prophylaxis.
Composition:
Ciprofloxacin-250 each film coated tablet contains
Ciprofloxacin USP 250 mg as hydrochloride.
Ciprofloxacin-500 each film coated tablet contains Ciprofloxacin
USP 500 mg as hydrochloride.
Ciprofloxacin-750 each film coated tablet contains
Ciprofloxacin USP 750 mg as hydrochloride.
Ciprofloxacin-XR 1 gm each film coated extended release
contains Ciprofloxacin USP 1 gm as hydrochloride.
Ciprofloxacin-250 powder for suspension: Each 5 ml
contains Ciprofloxacin USP 250 mg as hydrochloride.
Dosage and
Administration
Ciprofloxacin may be given orally without regard to
meals. Patients receiving Ciprofloxacin-should be well hydrated and should be
instructed to drink fluids liberally. Because of the risk of crystalluria. It
is recommended that the usual dosage of the drug should not be exceeded. For
the treatment of urinary tract infections, the usual adult oral dosage of
Ciprofloxacin for mild to moderate infections is 250 mg every 12 hours and the
adult dosage for complicated infections, caused by organisms not highly
susceptible to drug is 500 mg every 12 hours. The usual adult oral dosage of
Ciprofloxacin for infectious diarrhea is 500 mg every 12 hours. The usual adult
dosage for mild to moderate lower respiratory tract, skin and soft tissue or
bone and joint infections is 500 mg every 12 hours; a dosage of 750 mg every 12
hours may be needed, especially in bone and joint infections or when infections
are severe or complicated. In severe infections particularly due to
pseudomonas, staphylococcus and streptococci, the higher dosage of
Ciprofloxacin 750 tablet twice daily should be used. For surgical prophylaxis a
single dose of Ciprofloxacin 750 is given 60-90 minutes before the procedure.
For the treatment of uncomplicated urethral, endocervical or rectal gonorrhea
caused by penicillinase producing strains of neisseria gonorrhea (PPNG) or
non-penicillinase producing strains of the organism, adults should receive a
single 500 mg oral dose of Ciprofloxacin followed by oral doxycycline therapy
for possible coexisting Chlamydia infection in the treatment of chancroid, 500
mg orally twice daily for 3 day’s is required. The duration of therapy depends
on the type and severity of infection and should be determined by the clinical
and bacteriologic response of the patients. For most infections, therapy should
be continued for at least 48 hours after the patients become asymptomatic.
Theusual duration is 1-2 weeks but severe or complicated infections may require
more prolonged therapy, Ciprofloxacin-therapy may need to be continued for 4-6
weeks or longer for the treatment of bone and joint infections, infectious
diarrhea generally is treated for 3-7 day’s, although less prolonged therapy
may beadequate. Modification of the usual dosage Ciprofloxacin-generally is
unnecessary in patients with creatinine clearance greater than 50 ml/minute. In
patients with creatnine clearance of 50 ml/minute or less, doses and/or
frequency of administration of Ciprofloxacin should be modified in response to
the degree of renal impairment and the site and severity of infection. Adults
with creatinine clearance of 30-50 ml/minute can receive 250-500 mg of
Ciprofloxacin every 12 hours and adults with creatinine clearance of 5-29
ml/minute can receive 250-500 mg every 18 hours. Patients with severe
infections and severe renal impairment may be given 750 mg of Ciprofloxacin
every 12 or 18 hours. However, these patients should be monitored carefully and
serum Ciprofloxacin concentrations determined periodically.
Precaution and
Warning: It should be used with caution in patients
with suspected or known CNS disorders such as arteriosclerosis or epilepsy or
other factors which predispose to seizures and convulsion
Information for
patients:
Ciprofloxacin may be talen with or without meals and to
drink fluids liberally.
Concurrent administration of Ciprofloxacin should be
avoided with magnesium/aluminum antacids or sucralfate or with other products
containing calcium, iron or zinc. These products may be taken two hours after
or six hours before Ciprofloxacin.
Ciprofloxacin should not be taken concurrently with milk
or yogurt alone, since absorption of Ciprofloxacin may be significantly reduced.
Dietary calcium is a part of a meal, however, does not significantly affect the
Ciprofloxacin absorption.
Pregnancy, Lactation
and Children: Not to be used in pregnancy
and nursing stage. Though not recommended for the children where benefit
out-weighs risk a dosage of 7.5-15 mg/kg/day in two divided doses can be given
Contraindication: Patients with a history of hypersensitivity to
Ciprofloxacin or to other quiolones.
Adverse reaction: Adverse effects include nausea and other gastrointestinal disturbances, headache,
dizziness and skin rashes. Crystalluria has occurred with high doses.
Storage Condition: Store below 30 degree C. Protect from light and
moisture. Keep away from children’s reach.
Sunday, March 16, 2014
Cefradine
Description : Cefradine is a semi-synthetic and first generation cephalosporin that can be given both by mouth and by injection. It is a broad-spectrum bactericidal antibiotic active against both gram-positive and gram-negative bacteria. It is also highly active against most strains of penicillinase pro ducting staphylococci. It has a high degree of stability to many beta-lactamases.
Mode of action : Cefradine works by inhibiting bacterial cell wall synthesis. The final stage of peptidoglycan synthesis in the bacterial cell wall is a cross-linking reaction carried out by transpeptidase enzyme.Cefradine inhibits this transpeptidase enzyme. As aresult the cell wall of the bacterium is weekend, which then swells and ruptures.
Pharmacokinetics : The oral drug is well absorbed from the small intestine by cancer mediated active transport system. Plasma concentrations of 18-25 mg/l are achived after an oral dose of 500 mg and 24-35 mg/l after 1 gm, the peak plasma concentration being achieved around one hour after administration of the drug of the capsule. Serum concentrations after five minutes of intravenous administration were approximately 90 mg/l after 1 gm and 40 mg/l after 500 mg. The plasma half-life is 0.7 to 0.8 hour after oral administration and 0.3 hour after intravenous administration. Cefradine is not metabolized and has a large volume of distribution. Cefradine is excreted unchanged in urine.
Composition : Cefradine 250 mg capsules- Each capsule contains Cefradine USP
250 mg. Cefradine 500 mg capsules-Each capsule contains Cefradine USP 250 mg. Cefradine
powder for paediatric drops- After reconstitution each 5 ml contains Cefradine BP 250 mg. Cefradine
250 mg injection- Each vial contains
Cefradine USP 250 mg. Cefradine 500 mg injection- Each vial contains
Cefradine USP 500 mg and Cefradine 1 mg injection- Each vial contains Cefradine
USP 1 mg.
Indication
: Upper respiratory tract infections: Pharyngitis, tonsillitis,
sinusitis, otitis media, laryngo-tracheo bronchitis. Lower respiratory tract
infections: Acute and chronic bronchitis, lobar pneumonia, broncho pneumonia. Urinary
tract infections: Cystitis, urethritis, pyelonephritis, Skin and soft tissue
infections: Abscess, cellulitis, furunculosis, impetigo. Prophylaxis for
surgical procedures associated with high risk of disastrous consequences of
infection. Other serious infections caused by sensitive organisms in both
adults and children.
Dosage and
administration Cefradine: Cefradine may be given without regard to meals.
Oral: Adults: For urinary tract infections the usual dose is
500 mg four times daily or 1 gm twice daily; severe or chronic infections may
require larger doses. Prolonged intensive therapy is needed for complications
such as prostatitis and epididymtitis. For respiratory tract infections and
skin and soft tissue infections, the usual dose is 250 mg or 500 mg four times daily
or 1 gm twice daily depending on the severity and site of infections.
Children : The usual dose is 25 to 50 mg/kg/day in two to
four equally divided doses. For otitis media, the dose is 75 to 100 mg/kg/day
in divided doses every 6 to 12 hours. Maximum dose is 4 gm per day. Deep IM/IV
injection over 3-5 minutes or by IV infusion. Adults: 0.5 to 1 gm 6 hourly;
increased to 8 gm daily in severe infections. Children: 50 to 100 mg/kg daily
in 4 divided doses. For surgical prophylaxis, by deep IM/IV injection over 3 to
5 minutes, 1-2 gm immediately prior to surgery. Renal impairment dosage:
Patients not on dialysis : The following dosage schedule is suggested as a
guideline based on a dosage of 500 mg per 6 hours and on creatinine clearance.
Further modification in the dosage schedule may be required because of the
dosage selected and individual variation.
Creatinine
clearance (ml/min)
|
Dose
|
Time
interval
|
>20
|
500 mg
|
6 hrs
|
5-20
|
250 mg
|
6 hrs
|
<5
|
250 mg
|
50-70 hrs
|
Patients on chronic, intermittent haemodialysis:
250 mg at the start of haemodialysis; 250 mg 6-12 hours after
start; 250 mg 36-48 hours after start; 250 mg at start of next haemodialysis if
>30 hours after previous dose.
Direction
for use: Cefradine DS powder for suspension: For the suspension,
shake the bottle well before adding water. Then add 60 ml or 12 tea-spoonful of
boiled and cooled water to the bottle. Continue shaking the bottle gently until
the powder is mixed properly. Shake the bottle well before each use. Cefradine
powder for suspension: For the suspension, shake the bottle well before adding
water. Then add 75 ml or 15 tea-spoonful of boiled and cooled water to the
bottle. Continue shaking the bottle gently until the powder is mixed properly.
Shake the bottle well before each use. Cefradine powder for paediatric drops:
Before adding water, shake the bottle well. Then add 10 ml or 2 tea-spoonful of
boiled and cooled water to the bottle. Continue shaking the bottle gently until
the powder is mixed properly. Shake the bottle well before each use. Cefradine
250 mg and 500 mg injection: Intramuscular. Add 2 ml of water for injection to
250 mg or 500 mg vial and shake. Intravenous: Add 5 ml of water for injection
to 250 mg or 500 mg vial and shake. The solution should be slowly injected
directly into the vein over a 3 to 5 minutes period. Cefradine 1 gm injection:
Intramuscular: Add 4 ml of water for injection to 1 gm vial and shake.
Intravenous: Add 10 ml of water for injection to 1gm and shake. The solution
should be slowly injected directly into the vein over a 3 to 5 minutes period.
Contraindications: Patients with
known hypersensitivity to cephalosporins and with caution to those known to be
hypersensitive to penicillin, because cross-alergy can occur. Cefradine should
not be administered intrathecally.
Side
effects: Hypersensitivity phenomena are more likely in patients
with a history of allergy, asthma, hay lever or urticaria. Most side effects
have been encountered in about 7% of patients with oral cephalosporins,
principally nausea and diarhoea, skin rashes and vaginitis.
Use to
pregnancy and lactation: No teratogenicity has been demonstrated . Cefradine
should be used during pregnancy when clearly needed. Cefradine is excreted in
breast milk and should be used with caution in lactating mothers.
Precautions: In
penicillin-sensitive patients. Cefradine should be used with great caution.
Administer Cefradine with caution in the presence of markedly impaired renal
tunction.
Drug
Interactions : The cephalosporins are potentially nephrotoxic and may
enhance the nephrotoxicity of aminoglycoside antibiotics, such as gentamicin
and tobramycin. The nephrotoxicity of Cefradine is increased by furosemide and
one should be cautious about the use of any cephalosporin with furosemide and
ethacrynic and combinations with aminoglycosides may exert more potent
bactericidal action against some organisms then used alone.
Overdosage: There are
no well documented cases of overdose but severe nausea and diarhoea would be
expected. Convulsions may occur in patients receiving large doses of some
cephalosporins especially in patients with renal failure.
Storage : Store in a
cool and dry place, protected from light.