Flunarizine + Domperidone + Paracetamol Pharmacology

Flunarizine + Domperidone + Paracetamol

About Flunarizine + Domperidone + Paracetamol
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Mechanism of Action of Flunarizine + Domperidone + Paracetamol
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Pharmacokinets of Flunarizine + Domperidone + Paracetamol
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Onset of Action for Flunarizine + Domperidone + Paracetamol
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Duration of Action for Flunarizine + Domperidone + Paracetamol
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Half Life of Flunarizine + Domperidone + Paracetamol
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Side Effects of Flunarizine + Domperidone + Paracetamol
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Contra-indications of Flunarizine + Domperidone + Paracetamol
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Special Precautions while taking Flunarizine + Domperidone + Paracetamol
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Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Not recommended
Indications for Flunarizine + Domperidone + Paracetamol
Migraine prophylaxis
Interactions for Flunarizine + Domperidone + Paracetamol
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Typical Dosage for Flunarizine + Domperidone + Paracetamol
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Schedule of Flunarizine + Domperidone + Paracetamol
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Storage Requirements for Flunarizine + Domperidone + Paracetamol
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Effects of Missed Dosage of Flunarizine + Domperidone + Paracetamol
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Effects of Overdose of Flunarizine + Domperidone + Paracetamol
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Flunarizine

About Flunarizine
Calcium channel blocker and H1 blocker, Diphenyl Piperazine derivative, Antivertigo,Anti migraine, vasodilator, anticonvulsant.
Mechanism of Action of Flunarizine
Flunarizine is the diflourinated derivative of Cinnarizine. Flunarizine has H1 antihistaminic, sedative and calcium channel blocking actions. It is a cerebro selective calcium ion (Ca +2) channel blocker. It reduces the frequency of migraine attacks by reducing intracellular Ca +2 overload due to brain hypoxia and other causes. It inhibits the vasospasm induced by mediators such as serotonin and prostaglandins.
Antihistamines are the mainstay of the treatment of vertigo. Flunarizine suppresses end organ receptors or inhibit central cholinergic pathway in vestibular nuclei and produces antivertigo action


Pharmacokinets of Flunarizine
Absorption: Flunarizine is well absorbed after oral administration. Metabolism: Considerable amount undergoes hepatic metabolism.
Onset of Action for Flunarizine
60 minutes
Duration of Action for Flunarizine
3 weeks
Half Life of Flunarizine
19 days
Side Effects of Flunarizine
1.Nausea
2.Vomiting
3.Drowsiness
4.Headache
5.Abdominal disturbances
6.Weight gain
7.Insomnia
8.Depression
9.Rash
10.Tremor
11.Asthenia
12.Dry mouth
13.Extrapyramidal reactions
Contra-indications of Flunarizine
1.Hypersensitivity to Flunarizine
2.Depression
3.Parkinson`s disease
Special Precautions while taking Flunarizine
1. Patient should be cautioned against activities requiring mental alertness such as driving, operating machine or involving in any hazardous activities.
Pregnancy Related Information
Contraindicated.
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated.
Children Related Information
NULL
NEONATES: contraindicated
Indications for Flunarizine
1.Prophylaxis of Migraine
2.Prophylaxis of vertigo
3.Prophylaxis of vestibular disorders
4.Prophylaxis of peripheral and cerebrovascular disorders.
Interactions for Flunarizine
Phenytoin, Carbamazepine, Valproic acid: Decrease efficacy of flunarizine.
Typical Dosage for Flunarizine
Adult: 5 - 10 mg once daily in the evening.
Schedule of Flunarizine
H
Storage Requirements for Flunarizine
Store at 15 - 30 degree C. Protect from light and moisture. Keep out of the reach of children
Effects of Missed Dosage of Flunarizine
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 Flunarizine
Give supportive measures and symptomatic treatment. Drug can be removed from the body by gastric lavage or by emesis. Absorption of the drug can be reduced by administration of charcoal.

Domperidone

About Domperidone
Antidopaminergic, Motility stimulant,Piperidine derivative, Antiemetic, anti-vertigo.
Mechanism of Action of Domperidone
Domperidone is a potent dopamine receptor antagonist. It acts centrally and blocks the Dopamine receptor in the Chemoreceptor trigger zone and produces Antiemetic effect.
Domperidone acts peripherally in the gastrointestinal system and increases oesophageal peristalsis, oesophageal sphincter pressure and gastric motility. These all facilitates gastric emptying. Domperidone 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 Domperidone
Absorption: Domperidone is rapidly absorbed after oral administration. Since it undergoes first pass metabolism oral bioavailability is only 15 %. Distribution: It is widely distributed in the body in protein bound form. Metabolism: Domperidone undergoes metabolism in the liver. Excretion: It is excreted mainly in the faeces and also in the urine.
Onset of Action for Domperidone
30 - 60 minutes
Duration of Action for Domperidone
6 - 8 hours
Half Life of Domperidone
7.5 hours
Side Effects of Domperidone
1.Diarrhoea
2.Dry mouth
3.Galactorrhoea
4.Gynaecomastia
5.Skin rash
6.Abdominal discomfort
7.Dystonic reactions
Contra-indications of Domperidone
1.Hypersensitivity to Domperidone
2.Prolactin releasing pituitary tumour(prolactinoma)
3.Gastrointestinal obstruction
Special Precautions while taking Domperidone
1.Hepatic impairment
2.Renal impairment
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
Use with caution
NEONATES: contraindicated
Indications for Domperidone
1.Nausea and vomiting associated with gastrointestinal disorder and migraine.
2.Delayed gastric emptying of functional origin
3.As an Antiemetic in patient receiving cytotoxic drugs
4.Preanaesthetic medication

Interactions for Domperidone
Digoxin: Oral dose of digoxin needs to be reduced.
Aspirin, Paracetamol & Oral Diazepam: Increases absorption of these agents.
Anticholinergic agents: Antagonize the effects of domperidone.
Phenothiazines: CNS depression enhanced by domperidone.
Antimuscarinic agents and opioids: Antagonize GI effects of domperidone.
Suxamethonium: Neuromuscular blockade enhanced by domperidone.
Typical Dosage for Domperidone
Adults: 30 - 40 mg / day in 3 - 4 divided doses 30 minutes before meals and at bed time if required. After 2 weeks dose can be increased to 60 - 80 mg / day if needed.
Migraine: 20 mg by mouth may be taken up to every 4 hours with Paracetamol, as required up to a maximum of 4 doses in 24 hours.
Children: 300 mcg / kg body weight 3 - 4 times daily 30 minutes before meals and at bed time if required
Schedule of Domperidone
H
Storage Requirements for Domperidone
Store at room temperature (15 - 30 degree C). Protect from direct sun light and moisture
Effects of Missed Dosage of Domperidone
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 Domperidone
Give supportive measures and symptomatic treatment. Drug can be removed from the body by gastric lavage and absorption of the drug can be reduced by administration of activated charcoal. To control Extrapyramidal reactions give antiparkinsonian or anticholinergic agents.

Paracetamol

About Paracetamol
Acetanilide derivative, Non narcotic Analgesic,Antipyretic.
Mechanism of Action of Paracetamol
Paracetamol has analgesic and antipyretic action.
It is more active on cyclo-oxygenase enzyme in brain. Peripherally it is a poor inhibitor of prostaglandin synthesis.
Analgesic action: Paracetamol raises the pain threshold and produces analgesic effect.
Antipyretic action: Paracetamol lowers fever by direct action on the thermoregulatory centre in the Hypothalamus and block the effects of endogenous pyrogen.
Pharmacokinets of Paracetamol
Absorption: Paracetamol is rapidly and completely absorbed after oral administration.
Distribution: It is distributed mostly in the body in unbound form.
Metabolism: It is extensively metabolised in the liver.
Excretion: Excreted in the urine.
Onset of Action for Paracetamol
30 - 60 minutes
Duration of Action for Paracetamol
6 hours
Half Life of Paracetamol
1-4 hours
Side Effects of Paracetamol
1. Nausea
2. Abdominal distress
3. Allergic reactions
4. Rash
Contra-indications of Paracetamol
1. Hypersensitivity to Paracetamol
Special Precautions while taking Paracetamol
1. Hepatic impairment
2. Renal impairment
3. Hypertension
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
NEONATES : Contraindicated
Indications for Paracetamol
1. To relieve pain and fever
2. Acute gout
3. Migraine
Interactions for Paracetamol
Cholestyramine: Reduces absorption of paracetamol.
Charcoal: Activated, administered immediately reduces absorption of paracetamol.
Domperidone and metochlopramide: Enhance absorption of paracetamol.
Alcohol: Chronic excessive ingestion of alcohol potentiates hepatotoxicity of paracetamol.
Zidovudine: Effects zidovudine may be decreased.
Typical Dosage for Paracetamol
Adult:
500 - 1000 mg in 3 times daily
Maximum dose: 4 g / day
For migraine: 500 mg to be taken at the first sign of migraine attack and repeated 4 - 6 hourly until suppress mild attacks.
Children:
60 mg / kg body weight /day in 4 divided doses.
Schedule of Paracetamol
H
Storage Requirements for Paracetamol
Store at 15-30 degree C in a tightly closed container. Protect from heat and moisture. Keep out of the reach of children.
Effects of Missed Dosage of Paracetamol
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 Paracetamol
Give supportive measures and symptomatic treatment. Drug can be removed from the body by gastric lavage or by inducing emesis. Absorption of the drug can be reduced by administration of activated charcoal. N-acetylcysteine is the specific antidote for Paracetamol poisoning. Dose: 150 mg /kg body weight as IV infusion over 15 minutes followed by same dose over 20 hours.
Maintenance dose: 75 mg / kg orally every 4 - 6 hours for 2 - 3 days. Haemodialysis can be done in emergency conditions.

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