Primperan

Drugs , Gastrointestinal System / October 17, 2016

Class: Gastrointestinal System
Dosage Form: Various
Description: Antiemetic and gastroprokinetic
Stock: Available
Manufacturer: Sanofi Aventis

Composition:

Metoclopramide………..10 mg

Properties:

Pharmacodynamics
Metolcopramide is a dopamine antagonist neuroleptics, preventing nausea and vomiting by blocking dopamine sites.

Pharmacokinetics
Absorption
Metoclopramide is rapidly absorbed from the gastrointestinal tract. Bioavailability is generally 80%; however, this may vary between individuals due to hepatic first-pass effect.
Distribution
Metoclopramide is widely distirbuted into tissue. The volume of distribution is 2.2 to 3.4 l/kg. Plasma protein binding is low. The medicien crosses the placental barrier and passes into breast milk.
Metabolism
Metoclopramide underoges slight metabolism.
Excretion
Metoclopramide is mainly excreted in the urine in the unbound or subconjugated form. The elimination half-life is 5-6 hours. This value increases in the event of renal or hepatic impairment.

Indications:

Metoclopramide is indicated in:

  • Nausea and vomiting
  • Hiccup and migraines
  • Digestive dyskinesia
  • Radiologic investigations

Contraindicatons:

Metoclopramide is contraindicated in:

  • Hypersensitivity to metoclopramide or to one of the other ingredients in the product
  • If stimulation of gastrointestinal motility is hazardous to the patient: in the event of gastrointestinal bleeding, mechanical obstruction or gastrointestinal perforation
  • In patients having previously presented with tardive dyskinesia induced by neuroleptics or metoclopramide
  • In patients with known or suspected pheochromocytoma (apart from as a provocative test); serious hypertensive events have been reported with dopamine antagonists including certain benzamides in this patient category
  • In combination with dopamine agonists and selegiline with other medicinal products and other forms of interaction
  • Known history of methemoglobinemia with metoclopramide or NADH-cytochrome b5 reductase deficiency
  • Neurological undesirable effects (extrapyramidal syndrome) may develop, particularly in children and in youn adults
  • Since neurolpetic malignant syndrome has been reported in exceptional cases, treatment must be immediately discontinued in the event of unexplained hyperthermia or hyperthermia associated with other symptoms of malignant syndrome (pallor, vegetative disorders, impaired consciousness, muscular rigidity
  • In the event of vomiting, or partial/complete rejection of the dose administered, maintain the stipulated dosing interval before re-administering the medicinal product
  • In the even of profuse vomiting, it is essential to guard against dehydration

Drug Interactions:

1.Contraindicated Combination:

  • Dopamine agonists (levodopa, amantidine, apomorphine, bromocriptine, cabergoline, entacapone, lysuride, pergolide, piribedil, pramipexol, quinagolide, ropinirole)
  • Mutual antagonism of levodopa, dopamine agonists and neuroleptics. Use an antiemetic that does not given rise to any extrapyramidal effects

2. Combination to be avoided:

  • Alcohol: Alcohol increases the sedative effect of neuroleptics. Driving and using machines may be hazardous due to impaired vigilance. Avoid consumption of alcoholic beverages and intake of medicinal products containing alcohol.

3. Combination to be taken into account:

  • Antihypertensive agents (all types): Antihypertensive effect and increased risk of orthostatic hypotension (additive effect).
  • Other central nervous system depressants: Morphine derivatives (analgesics, antitussive agents and replacement treatments), barbiturates, benzodiazepines, anxiolytics other than benzodiazepines, neuroleptics, sedative antidepressants (amitriptyline, doxepine, mianserin, mirtazapine, trimipramine) sedative H1-antihistamines, centrally acting antihypertensive agents, baclofen, thalidomide, pizotifen. Increased CNS depression. Driving and using machines may be dangerous due to impaired vigilance.
  • Beta-blockers in the event of cardiac insufficiency (bisoprolol, carvedilol, metoprolol): Vasodilator effect and risk of hypotension, particularly orthostatic hypotension (additive effect).

Side Effects:

In certain patients previously treated with neuroleptics or presenting hypersensitivity to this type of product, localized or generalised muscle spasms may occur, particularly in children, but these are spontaneously completely reversible after treatment discontinuation.

1. Central Nervous System and Psychiatric Disorders:

  • Extrapyramidal symptoms:
    • Increased risk of onset in children and young adults and/or when the recommended dose is exceeded.
    • Symptoms include acute dystonia manifested by abnormal movements of the head and neck (facial spasms, trismus, oculogyric crisis, ocular revulsion, protrusion of the tongue, swallowing difficulties, dysarthria, torticollis), generalized hypertonia, or even opisthotonos.
    • Reactions generally occur at the beginning of treatment, between 1 and 3 hours after the last dose
    • Symptoms may appear after a single administration
    • If extrapyramidal symptoms develop, it is advisable to discontinue treatment with metoclopramide
    • Effects are generally fully reversible on treatment discontinuation; however, symptomatic treatment may be necessary (benzodiazepine in children, benzodiazepines and/or anticholinergic antiparkinsonians in adults).
  • Tardive dyskinesia: During prolonged traetment, particularly in elderly patients
  • Drowsiness, fatigue, dizziness, more rarely headache, insomnia
  • Tendency towards depression
  • In exceptional cases, neuroleptic malignant syndrome

b) Gastrointestinal disorders:

  • Diarrhea and intestinal gas

c) Hematological disorders:

  • Very rare cases of methemoglobinemia, possibly due to NADH-cytochrome b5-reductase deficiency, have been reported, particularly in newborn infants
  • Very rare cases of sulfhemoglobinemia have been reported, mainly during concomitant administration of sulphate-releasing medicinal rpdocuts at high doses

d) Endocrine disorders:

  • Occasionally symptomatic hyperprolactinemia (amenorrhea, galactorrhea, gynecomastia) during prolonged treatment
  • Moderate sweating

e) General disorders:

  • Allergic reactions including immediate hypersensitivity reactions: urticaria, angio-edema, anaphylactic shock

f) Cardiovascular disorders:

  • Hypotension, particularly with injection forms
  • These reactions generally occur at the beginning of treatment, between 1 and 3 hours after the last dose
  • Symptoms may appear after a single administration
  • If extrapyramidal symptoms develop, it is advisable to discontinue treatment with metoclopramide
  • These effects are generally fully reversible on treatment discontinuation; however, symptomatic treatment may be necessary (benzodiazepines in children, benzodiazepines and/or anticholinergic antiparkinsonians in adults)

Dosage and Administration:

1. Adults: 

  • Tablets: 1/2 to 1 tablet three times per day before meals
  • Injectable solution: Acute syndromes, one IM or IV injection repeated if necessary
  • Syrup: 1-2 teaspoonfuls (5 ml = 5 mg) three times per day before meals
  • Suppositories: 1-2 suppositories (20 mg) per day

2. Children:

  • Injectable solution: Over 20 kg, half the adult dose
  • Syrup: Drops, 0.5 mg/kg/day, (Use only the drop-counter included in the package)
  • Suppositories: For children over 20 kg, 0.5 mg/kg/day

Overdosage:

Symptoms
No fatalities have been observed following massive intake of metoclopramide, either accidental or as a suicide attempt. Moderate consciousness disorders or extrapyramidal syndromes may be observed.

Treatment
Treatment of extrapyramidal syndrome, which may or may not be related to overdose, is purely symptomatic (benzodiazepines in children, benzodiazepines and/or anticholinergic antiparkinsonians in adults). Administration may be repeated in order to prevent symptoms from recurring.
In the event of methemoglobinemia, methylene blue at a dose of 1 mg/kg has been effective when administered as a slow infusion.

Pregnancy and Lactation:

Pregnancy
Animal studies have not demonstrated any teratogenic effects.
In a clinical context, the use of metoclopramide during pregnancy does not appear to have evidenced any particular teratogenic or fetotoxic effects to date. However, additional studies are necessary in order to evaluate the effects of exposure during pregnancy.
Consequently, use of metoclopramide should only be envisaged during pregnancy if necessary.
A potential extrapyramidal syndrome cannot be excluded in newborn infants whose mothers had received long-term treatment with high-dose metoclopramide, by analogy with other neuroleptics.
Consequently, it would seem reasonable to attempt to limit the prescribed doses and treatment duration for products with a similar pharmacological activity during pregnancy.
Monitoring of newborn neurological function is justified in the event of prolonged and/or high-dose treatment, and/or treatment close to the term of pregnancy.

Lactation
Breast-feeding is possible in the event of brief treatment with the medicinal product, for example, in the context of vomiting following “Caesrean section”, if the infant was born at fill=term and in good health. Breast-feeding is not recommended in the event of premature birth or prolonged or high-dose treatment.

Warnings:

Neurological undesirable side effects (extrapyramidal syndrome) may develop, particularly in children and young adults.
Since neurological malignant syndrome has been reported in exceptional cases, treatment must be immediately discontinued in the event of unexplained hyperthermia or hyperthermia associated with other symptoms of malignant syndrome (pallor, vegetative disorders, impaired consciousness, muscular rigidity).
In the event of vomiting, or partial/complete rejection of the dose administered, maintain the stipulated dosing interval before re-administering the medicinal product.
In the even of profuse vomiting, it is essential to guard against dehydration. The patient may be rehydrated orally using “sweet-saline” solutions (oral rehydration solutions) given in small quantities at regular intervals.
Cases of methemoglobinemia, possibly due to NADH-cytochrome b5 reductase deficiency, have been reported. In such an event, treatment must be immediately and definitvely discontinued, and appropriate measures implemented.
Due to the presence of lactose, this medicinal product is contraindicated in the event of congenital galactosemia, glucose/galactose malabsorption syndrome or lactase deficiency.
Use of this medicinal product is not recommended in epileptic patients (increased frequency and intensity of fits).
In the event of renal or hepatic impairment, it is advisable to reduce the dosage.

Packaging:

Box of 20 tablets containing 10 mg of metoclopramide hydrochloride.
Box of 12 ampoules for injection, each containing 10 mg of metoclopramide hydrochloride.
[WITHDRAWN] Bottle of 120 ml of syrup each teaspoonful containing 5 mg. [WITHDRAWN]
Box of 6 suppositories each containing 20 mg of metoclopramide, for adults.

Storage:

Store at room temperature, below 25°C.

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