Domperidone + Paracetamol + Tramadol Pharmacology

Domperidone + Paracetamol + Tramadol

About Domperidone + Paracetamol + Tramadol
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Mechanism of Action of Domperidone + Paracetamol + Tramadol
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Pharmacokinets of Domperidone + Paracetamol + Tramadol
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Onset of Action for Domperidone + Paracetamol + Tramadol
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Duration of Action for Domperidone + Paracetamol + Tramadol
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Half Life of Domperidone + Paracetamol + Tramadol
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Side Effects of Domperidone + Paracetamol + Tramadol
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Contra-indications of Domperidone + Paracetamol + Tramadol
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Special Precautions while taking Domperidone + Paracetamol + Tramadol
N/A
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Not recommended
Children Related Information
Use with caution
Indications for Domperidone + Paracetamol + Tramadol
1.All painful inflammatory conditions related to musculoskeletal tissue
2.Inflammatory dental condition
3.Dysmenorrhoea
Interactions for Domperidone + Paracetamol + Tramadol
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Typical Dosage for Domperidone + Paracetamol + Tramadol
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Schedule of Domperidone + Paracetamol + Tramadol
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Storage Requirements for Domperidone + Paracetamol + Tramadol
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Effects of Missed Dosage of Domperidone + Paracetamol + Tramadol
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Effects of Overdose of Domperidone + Paracetamol + Tramadol
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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.

Tramadol

About Tramadol
A synthetic analogue of codein, Centrally acting Narcotic Analgesic.
Mechanism of Action of Tramadol
It is centrally acting synthetic drug. Chemically it is not related to the opiates but it act on the Opioid receptors present in the CNS. It has weak agonistic action on mu Opioid receptors, it cause analgesia. Part of this analgesic effect is due to the inhibition of norepinephrine and serotonin reuptake inhibition. However it has agonistic action on mu receptors, respiratory depression and gastrointestinal effects are not prominent.
Pharmacokinets of Tramadol
Absorption-Absorbed well after oral, intravenous and other parenteral application.
Distribution-Widely distributed in the body, about 20% bound to the plasma protein. It may cross the placenta.
Metabolism-It is metabolized in the liver by O-demethylation; N-demethylation, glucoronidation or sulfation to its metabolites. Mono-O-desmethylate is its active metabolite.
Excretion - Excreted 30% as unchanged form and 60% as its metabolites via urine.
Onset of Action for Tramadol
30 to 60 hrs
Duration of Action for Tramadol
8 to 12 hrs
Half Life of Tramadol
N/A
Side Effects of Tramadol
1. Dizziness
2. Weakness
3. Headache
4. Anxiety
5. Agitation
6. Drowsiness
7. Blurred vision
8. Stomach upset
9. Vomiting
10. Diarrhea
11. Constipation
12. Itching
13. Sweating
14. Flushing
15. Dry mouth
Contra-indications of Tramadol
1. Hypersensitivity to this drug
2. Acute alcoholic intoxification
3. Hypnotics
4. With centrally acting analgesics
5. With psychotropic drug
6. With Opioid drug
Special Precautions while taking Tramadol
1. Head injury
2. Acute abdominal conditions
3. Seizures
4. Respiratory depression
5. Renal failure
6. Hepatic failure
7. Physical dependence on Opioids
Pregnancy Related Information
May be used
Old Age Related Information
Use with caution
Breast Feeding Related Information
May be used
Children Related Information
May be used
Indications for Tramadol
1. Post operative pain
2. Arthralgia
3. Musculoskeletal pain
4. Low back pain
5. Pain associated with other reasons
Interactions for Tramadol
Carbamazepine: A significant increase in Tramadol metabolism.
Hypnotics, Tranquilizers and other CNS depressants: Sedative effects potentiated.
MAOIs: Fatal interaction occurs.
Opioid analgesics like Buprenorphine, Butorphanol and Pentazocine: May precipitate withdrawl symptoms.
Tranquilizers: Analgesia potentiated.
Typical Dosage for Tramadol
Oral-
Adults - 50 to 100mg every 4 to 6 hrs or twice daily.
Intravenous-
50 to 100 mg given every 4 to 6 hrs.
Rectal-
100 mg suppository 4 times daily.
Schedule of Tramadol
N/A
Storage Requirements for Tramadol
Store at room temperature in a tightly closed container and away from heat & moisture. Keep out of reach of children.
Effects of Missed Dosage of Tramadol
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 Tramadol
Establish artificial respiratory exchange. Naloxone administration cannot relieve all the symptoms produced by tramadol. Haemodialysis can remove a small fraction of drug from the body. Provide symptomatic and supportive treatment.

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