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- Pharmacology For Flunarizine + Domperidone + Paracetamol
Flunarizine + Domperidone + Paracetamol Pharmacology
Flunarizine + Domperidone + Paracetamol
About Flunarizine + Domperidone + ParacetamolN/AMechanism of Action of Flunarizine + Domperidone + ParacetamolN/APharmacokinets of Flunarizine + Domperidone + ParacetamolN/AOnset of Action for Flunarizine + Domperidone + ParacetamolN/ADuration of Action for Flunarizine + Domperidone + ParacetamolN/AHalf Life of Flunarizine + Domperidone + ParacetamolN/ASide Effects of Flunarizine + Domperidone + ParacetamolN/AContra-indications of Flunarizine + Domperidone + ParacetamolN/ASpecial Precautions while taking Flunarizine + Domperidone + ParacetamolN/APregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationNot recommendedIndications for Flunarizine + Domperidone + ParacetamolMigraine prophylaxisInteractions for Flunarizine + Domperidone + ParacetamolN/ATypical Dosage for Flunarizine + Domperidone + ParacetamolN/ASchedule of Flunarizine + Domperidone + ParacetamolN/AStorage Requirements for Flunarizine + Domperidone + ParacetamolN/AEffects of Missed Dosage of Flunarizine + Domperidone + ParacetamolN/AEffects of Overdose of Flunarizine + Domperidone + ParacetamolN/AFlunarizine
About FlunarizineCalcium channel blocker and H1 blocker, Diphenyl Piperazine derivative, Antivertigo,Anti migraine, vasodilator, anticonvulsant.Mechanism of Action of FlunarizineFlunarizine 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 FlunarizineAbsorption: Flunarizine is well absorbed after oral administration. Metabolism: Considerable amount undergoes hepatic metabolism.Onset of Action for Flunarizine60 minutesDuration of Action for Flunarizine3 weeksHalf Life of Flunarizine19 daysSide Effects of Flunarizine1.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 Flunarizine1.Hypersensitivity to Flunarizine
2.Depression
3.Parkinson`s disease
Special Precautions while taking Flunarizine1. Patient should be cautioned against activities requiring mental alertness such as driving, operating machine or involving in any hazardous activities.Pregnancy Related InformationContraindicated.Old Age Related InformationUse with cautionBreast Feeding Related InformationContraindicated.Children Related InformationNULL
NEONATES: contraindicatedIndications for Flunarizine1.Prophylaxis of Migraine
2.Prophylaxis of vertigo
3.Prophylaxis of vestibular disorders
4.Prophylaxis of peripheral and cerebrovascular disorders.
Interactions for FlunarizinePhenytoin, Carbamazepine, Valproic acid: Decrease efficacy of flunarizine.Typical Dosage for FlunarizineAdult: 5 - 10 mg once daily in the evening.Schedule of FlunarizineHStorage Requirements for FlunarizineStore at 15 - 30 degree C. Protect from light and moisture. Keep out of the reach of childrenEffects of Missed Dosage of FlunarizineTake 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 FlunarizineGive 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 DomperidoneAntidopaminergic, Motility stimulant,Piperidine derivative, Antiemetic, anti-vertigo.Mechanism of Action of DomperidoneDomperidone 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 DomperidoneAbsorption: 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 Domperidone30 - 60 minutesDuration of Action for Domperidone6 - 8 hoursHalf Life of Domperidone7.5 hoursSide Effects of Domperidone1.Diarrhoea
2.Dry mouth
3.Galactorrhoea
4.Gynaecomastia
5.Skin rash
6.Abdominal discomfort
7.Dystonic reactions
Contra-indications of Domperidone1.Hypersensitivity to Domperidone
2.Prolactin releasing pituitary tumour(prolactinoma)
3.Gastrointestinal obstruction
Special Precautions while taking Domperidone1.Hepatic impairment
2.Renal impairment
Pregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationUse with cautionChildren Related InformationUse with caution
NEONATES: contraindicatedIndications for Domperidone1.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 DomperidoneDigoxin: 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 DomperidoneAdults: 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 DomperidoneHStorage Requirements for DomperidoneStore at room temperature (15 - 30 degree C). Protect from direct sun light and moistureEffects of Missed Dosage of DomperidoneTake 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 DomperidoneGive 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 ParacetamolAcetanilide derivative, Non narcotic Analgesic,Antipyretic.Mechanism of Action of ParacetamolParacetamol 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 ParacetamolAbsorption: 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 Paracetamol30 - 60 minutesDuration of Action for Paracetamol6 hoursHalf Life of Paracetamol1-4 hoursSide Effects of Paracetamol1. Nausea
2. Abdominal distress
3. Allergic reactions
4. Rash
Contra-indications of Paracetamol1. Hypersensitivity to ParacetamolSpecial Precautions while taking Paracetamol1. Hepatic impairment
2. Renal impairment
3. Hypertension
Pregnancy Related InformationUse with cautionOld Age Related InformationUse with cautionBreast Feeding Related InformationUse with cautionChildren Related InformationUse with caution
NEONATES : Contraindicated
Indications for Paracetamol1. To relieve pain and fever
2. Acute gout
3. Migraine
Interactions for ParacetamolCholestyramine: 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 ParacetamolAdult:
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 ParacetamolHStorage Requirements for ParacetamolStore 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 ParacetamolTake 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 ParacetamolGive 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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