Metronidazole + Loperamide Pharmacology

Metronidazole + Loperamide

About Metronidazole + Loperamide
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Mechanism of Action of Metronidazole + Loperamide
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Pharmacokinets of Metronidazole + Loperamide
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Onset of Action for Metronidazole + Loperamide
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Duration of Action for Metronidazole + Loperamide
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Half Life of Metronidazole + Loperamide
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Side Effects of Metronidazole + Loperamide
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Contra-indications of Metronidazole + Loperamide
N/A
Special Precautions while taking Metronidazole + Loperamide
N/A
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
N/A
Indications for Metronidazole + Loperamide
Infectious diarrhea
Interactions for Metronidazole + Loperamide
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Typical Dosage for Metronidazole + Loperamide
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Schedule of Metronidazole + Loperamide
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Storage Requirements for Metronidazole + Loperamide
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Effects of Missed Dosage of Metronidazole + Loperamide
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Effects of Overdose of Metronidazole + Loperamide
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Metronidazole

About Metronidazole
A nitroimidazole antibiotic, Anti-infective, Antiprotozoal,amebicide.
Mechanism of Action of Metronidazole
Metronidazole is nitro imidazoles which have broad spectrum cidal activity against Protozoa and some anaerobic bacteria. Its selective toxicity to anaerobic microbes involves 1. Drug enters the cell by diffusion, 2. Nitro group of drug is reduced by redox proteins present only in anaerobic organisms to reactive nitro radical which exerts cytotoxic action by damaging DNA and other critical biomolecules. 3. DNA helix destabilization & strand breakage has been observed.
Pharmacokinets of Metronidazole
Absorption: Well absorbed orally, Distribution: Widely distributed,
Metabolism: Metabolized in liver by oxidation & glucuronide conjugation, Excretion: Excreted in urine.
Onset of Action for Metronidazole
1 to 2 days
Duration of Action for Metronidazole
8hours.
Half Life of Metronidazole
8 hours.
Side Effects of Metronidazole
1.Anorexia.
2.Metallic taste
3.Nausea
4.Vomiting
5.Diarrhoea
6.Headache
7.Looseness of stool.
8.Peripheral neuropathy &CNS effects.
9.Mutagenesis.
10.Radiosensitisation.
11.Transient leucopenia
12.Dry mouth
13.Abdominal distress
14.Dizziness
15.Vertigo
16.Thrombophlebitis at site of injection
17.Ototoxicity
Contra-indications of Metronidazole
1.Hypersensitivity to the drug
2.Blood dyscrasias
3.CNS disorders
Special Precautions while taking Metronidazole
1.Renal impairment
2.Hepatic impairment
3.Alcoholic cirrhosis
4.Use cautiously along with other hepatotoxic drugs & In visual field changes
Pregnancy Related Information
Use with caution
First trimester:contra indicated
Old Age Related Information
May be used.
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
Neonates: Contraindicated
Indications for Metronidazole
1.Amoebiasis
2.Giardiasis
3.Trichomonas vaginitis
4.Pseudo membranous enterocolitis
5.Anaerobic bacterial infections after surgery, Brain abscess, & Endocarditis
6.Helicobacter pylori infections
7.Ulcerative gingivitis
Interactions for Metronidazole
Warfarin & other coumarin anticoagulants: Potentiates the anticoagulant effect resulting in increased prothrombin time.
Alcohol: A disulfiram-like reaction. Abdominal cramps, nausea, vomiting, headache & flushing.
Disulfiram: Acute psychotic reaction or confusional state.
Phenobarbital & Phenytoin: Increased metabolism of metronidazole resulting in decreased efficacy.
Lithium: Increased lithium levels and toxicity.
Flurouracil: Increased toxicity of flurouracil.
Lab tests: May interfere with chemical analysis for AST,SGOT, ALT, SGPT, LDH, triglycerides and hexokinase glucose. Zero values may occur.
Typical Dosage for Metronidazole
Adult
Amoebiasis:400 to 800 mg 8hourly for 5 to 10days depending up on the severity of infection
In severe infections and liver abscess: 1gm as slow I.V. infusion followed by 0.5 gm twice daily till oral therapy is started
Giardiasis:200mg 8hourly for 1week or 2gm/day for 3days or I.V.500mg thrice daily
Trichomonas vaginitis: 400mg 8 hourly for a week or 2gm once daily for a week.
Male partner should be concurrently treated with the drug
Pseudo membranous enterocolitis:800 mg 8hourly
Anaerobic bacterial infections after surgery, Brain abscess, & Endocarditis:400 to 800 mg 8hourly
In severe cases: 15mg/kg I.V. infusion for 1hour followed by 7.5mg/kg 4 times daily till oral therapy is substituted
Helicobacter pylori infections:400mg 8hourly along with amoxicillin/clarithromycin and a proton pump inhibitor
Ulcerative gingivitis:200 to 800mg 8hourly
Children
Amoebiasis: 30 to 50mg/kg/day for 5to10 days.
Giardiasis:10 to 15mg/kg/day thrice daily
Children (below 12years): 7.5mg/kg I.V.
Schedule of Metronidazole
H
Storage Requirements for Metronidazole
Store in a well closed container in a cool dark place. Keep out of the reach of children.
Effects of Missed Dosage of Metronidazole
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Metronidazole
Treatment is supportive & symptomatic. Drug is removed by induced emesis, gastric lavage, and administration of activated charcoal & use of cathartics. For controlling seizures diazepam & phenytoin may be used.

Loperamide

About Loperamide
A synthetic piperidine derivative, Opioid, Antidiarrhoeal, Analgesic.
Mechanism of Action of Loperamide
Loperamide is a mu receptor agonist. It inhibits the release of Acetylcholine on myenteric plexus in the gastrointestinal tract. This results in slowing intestinal motility and reduces peristalsis and increase intestinal transit time. This will results in increased absorption of water from fecal matter. Loperamide also has a direct action on intestinal smooth muscle. It does not have any effect on central nervous system.
Pharmacokinets of Loperamide
Absorption: Loperamide is poorly absorbed after oral administration
Distribution: It is widely distributed mainly in protein bound form
Metabolism: Absorbed drug undergoes metabolism in the liver
Excretion: It is excreted mainly in the faeces and small amount in the urine.
Onset of Action for Loperamide
1 - 2 hours.
Duration of Action for Loperamide
1 day
Half Life of Loperamide
7 - 14 hours
Side Effects of Loperamide
1.Dry mouth
2.Abdominal pain
3.Nausea
4.Vomiting
5.Gastric discomfort
6.Drowsiness
7.Dizziness
8.Tiredness
9.Constipation
10.Allergic reaction
11.Toxic megacolon
Contra-indications of Loperamide
1.Hypersensitivity to Loperamide
2.Severe diarrhoea where inhibition of peristalsis is not desirable
3.Fever
4.Bloody stool diarrhoea
5.Pseudomembranous enterocolitis
Special Precautions while taking Loperamide
1.Hepatic impairment
2.Acute ulcerative colitis
3.Crohn`s disease
4.Intestinal stasis
5.Pyloric obstruction
6.Urinary bladder neck obstruction
7.Gastric retentions
8.Use caution while driving vehicle or operating machine or performing activities requiring mental alertness
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Below 2 years: contraindicated
NEONATES: contraindicated
Indications for Loperamide
1.Diarrhoea
Interactions for Loperamide
N/A
Typical Dosage for Loperamide
Adult (Oral): Initial dose: 4 mg followed by 2 mg after each loose motion. Maintenance dose: 6 - 8 mg daily
Maximum dose: 16 mg / day
Children:
2 - 5 years: 3 mg / day in 3 divided doses
6 - 8 years: 4 mg / day in 2 divided doses
8 - 12 years: 6 mg / day in 3 divided doses
Schedule of Loperamide
H
Storage Requirements for Loperamide
Store the drug at 15 - 30 degree C in a tightly closed container. Protect from heat and light.
Effects of Missed Dosage of Loperamide
Do not apply if it is taken as to control diarrhoea.
If it is taken as a regular schedule then take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.

Effects of Overdose of Loperamide
Give supportive measures and symptomatic treatment. Drug can be removed from the body by gastric lavage. Absorption of the drug can be reduced by administration of activated charcoal. Respiratory depression can be treated with Naloxone.

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