Metoclopramide +Simethicone Pharmacology

Metoclopramide +Simethicone

About Metoclopramide +Simethicone
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Mechanism of Action of Metoclopramide +Simethicone
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Pharmacokinets of Metoclopramide +Simethicone
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Onset of Action for Metoclopramide +Simethicone
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Duration of Action for Metoclopramide +Simethicone
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Half Life of Metoclopramide +Simethicone
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Side Effects of Metoclopramide +Simethicone
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Contra-indications of Metoclopramide +Simethicone
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Special Precautions while taking Metoclopramide +Simethicone
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Pregnancy Related Information
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Old Age Related Information
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Breast Feeding Related Information
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Children Related Information
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Indications for Metoclopramide +Simethicone
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Interactions for Metoclopramide +Simethicone
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Typical Dosage for Metoclopramide +Simethicone
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Schedule of Metoclopramide +Simethicone
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Storage Requirements for Metoclopramide +Simethicone
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Effects of Missed Dosage of Metoclopramide +Simethicone
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Effects of Overdose of Metoclopramide +Simethicone
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Metoclopramide

About Metoclopramide
It is a dopamine antagonist - antiemetic gastroprokinetic agent.
Mechanism of Action of Metoclopramide
Metoclopramide acts through both serotonergic and dopaminergic receptors. Metoclopramide binds to Serotonin (5 HT3 &5HT4) and Dopamine (D2) receptor.
Antiemetic action: Metoclopramide inhibits Dopamine receptor in the chemoreceptor trigger zone and produces antiemetic action.
Intestinal motility modifying action: The binding of Metoclopramide on 5HT4 receptor will activate interneuron and enhance the release of acetylcholine innervating the smooth muscles. This produces gastric emptying and enhances lower esophageal sphincter tone.
Migraine: Metoclopramide is used in migraine to relieve nausea and vomiting
Anaesthetic adjuncts: It is used preoperatively in order to reduce the post operative vomiting.
Pharmacokinets of Metoclopramide
Absorption: Metoclopramide is rapidly and well absorbed after oral administration. Distribution: It is extensively distributed to tissues and fluids, brain.
Metabolism: Only a small amount undergoes hepatic metabolism. Excretion: It is excreted mainly in urine and faeces.
Onset of Action for Metoclopramide
Oral: ? - 1 hour.
IM: 10 - 15 minutes
IV: 1 - 3 minutes
Duration of Action for Metoclopramide
1-2 hours.
Half Life of Metoclopramide
3 - 6 hour.
Side Effects of Metoclopramide
1.Drowsiness
2.Confusion
3.Constipation
4.Muscle spasm
5.Tremor
6.Bronchospasm
7.Bradycardia
8.Fatigue
9.Headache
10.Dizziness
11.Nervousness
12.Sedation
13.Nausea
14.Rash
Contra-indications of Metoclopramide
1.Hypersensitivity to Metoclopramide
2.Gastrointestinal haemorrhage
3.Mechanical obstruction
4.Pheochromocytoma
5.Epilepsy
6.Parkinsonism
7.Pyloric stenosis
8.Previous history of dystonia
Special Precautions while taking Metoclopramide
1. Hypertension
2. Depression
3. Renal impairment
4. Hepatic impairment
5. Use with caution while driving vehicles, operating machines and people involving any other dangerous activities
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
NEONATES: contraindicated
Indications for Metoclopramide
1. Nausea and vomiting (except motion sickness)
a)associated with various gastrointestinal disorders and migraine
b) Nausea and vomiting associated with cytotoxic chemotherapy or radiotherapy.
c) Post operative nausea and vomiting
2. Treatment of delayed gastric motility
3. Gastroesophageal reflux
4. Diagnostic procedure in gastroenterology

Interactions for Metoclopramide
Anticholinergic drugs and narcotic analgesics: Effects on GI motility are antagonised by these drugs.
Alcohol, sedatives, hypnotics, narcotics or tranquilizers: Additive sedative effect may occur.
Digoxin, Cimetidine: Absorption of these drugs decreased.
Acetaminophen, Aspirin: The absorption of these agents increased.
Phenothiazines, Butyrophenone, Lithium and Thioxanthine drugs: May potentiate extrapyramidal effects.
Bromocriptine: Antagonism of hypoprolactinaemic effect of bromocryptine.
Cyclosporine: May lead to increased cyclosporine absorption, possibly increasing immunosupressive and toxic effect.
Succinylcholine: Metoclopramide may increase the neuromuscular blocking effects of succinylcholine.
Typical Dosage for Metoclopramide
Adult:
ORAL: 15 - 30 mg / day in 3 divided doses.
Treatment of delayed gastric motility: 10 mg to be taken 30 minutes before each meal and at bed time for3 months. Drug is given depending upon the symptom being treated and clinical response.
Gastroesophageal reflux: 10 - 15 mg 4 times a day, drug to be taken half an hour before each meal and at bed time.
INJECTION:
Post operative nausea and vomiting: 10 - 20 mg IM at the end of surgical procedure and repeat the dose every 4 - 6 hours if needed
Nausea and vomiting associated with cytotoxic chemotherapy or radiotherapy: 2 - 4 mg / kg as IV infusion over 15 - 30 minutes.
Maintenance dose: 3 - 5 mg / kg given over 8 hours
Maximum dose: 10 mg / kg / day.
Children:
ORAL: 0.4 mg / kg / day in 4 divided doses.
Schedule of Metoclopramide
H
Storage Requirements for Metoclopramide
Store at 15 - 30 degree C in a tightly closed container. Protect from heat and light.
Effects of Missed Dosage of Metoclopramide
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 Metoclopramide
Give supportive measures and symptomatic treatment. Extrapyramidal effects may be controlled by administration of antimuscarinic or antiparkinsonian agents or antihistamine with antimuscarinic activity

Simethicone

About Simethicone
Oral anti-foaming agent, Silicones, Antiflatulent.
Mechanism of Action of Simethicone
This anti-gas (anti-flatulence) medication acts in the stomach and intestines to change the surface tension of gas bubbles, enabling smaller bubbles to join together into bigger bubbles. It results elimination of gas more easily by belching or passing flatus.
Pharmacokinets of Simethicone
Excretion- Excreted through feces.
Onset of Action for Simethicone
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Duration of Action for Simethicone
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Half Life of Simethicone
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Side Effects of Simethicone
1. Bloating
2. Constipation
3. Diarrhea
4. Gas
5. Heartburn
Contra-indications of Simethicone
1. Hypersensitivity to the drug
2. Liver disease
3. Kidney disease
4. Serious illness
Special Precautions while taking Simethicone
1.Swallow the tablets and capsules with a full glass of water.
2.Chew the chewable tablets thoroughly before swallowing.
3.Shake the drops well before using them.
4.To make administration easier, the drops can be mixed with 30 ml (2 tablespoons) of water or another liquid.
Pregnancy Related Information
Use with caution
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
Use with caution
Indications for Simethicone
1. Abdominal pain which is due to excessive gas in the digestive tract
2. Before gastroscopy or radiography of the bowel
Interactions for Simethicone
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Typical Dosage for Simethicone
Oral-
Adults and teenagers-
60 -125mg four times a day, after meals and at bedtime. Not more than 500 mg should be taken in twenty-four hours.
Chewable tablets:
Adults and teenagers-
40 -125 mg four times a day, after meals and at bedtime or 150 mg three times a day, after meals. Not more than 500 mg should be taken in twenty-four hours.
Suspension:
Adults and teenagers-
40 -95 mg four times a day, after meals and at bedtime. Not more than 500 mg should be taken in twenty-four hours.
Schedule of Simethicone
N/A
Storage Requirements for Simethicone
Stored at room temperature (15-30?C) away from moisture and heat.
Effects of Missed Dosage of Simethicone
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 Simethicone
Give symptomatic and supportive treatment.

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