Pentazocine
Pentazocine is a narcotic analgesic, with mixed agonist and antagonist activity. Pentazocine is more potent than codeine but less effective than morphine. Significant analgesia occurs within 15- 30 min. after oral administration, 15-20 min. after IM injection, and 2-3 min. after IV injection. Onset, duration of action and degree of pain relief are related both to dose and severity of pretreatment pain. it also has some activity as a narcotic antagonist like Naloxone. its derivatives are Pentazocine (HCl) and Pentazocine Lactate belongs to class of opioid or narcotic analgesic used to treat moderate to severe pain.
Primary Characteristics
Pentazocine is also known as Pentazocine (HCl), Pentazocine Lactate.
It is of Synthetic origin and belongs to Opioid.
It belongs to OPIATE agonist pharmacological group on the basis of mechanism of action. It is also classified under Analgesics and Anti-inflammatory Agents .
Molecular Weight: 321.9 · pKa: 8.7, 10.0 · Solubility in Water: 1 in 30 · Solubility in Alcohol: 1 in 16 · Non-proprietary name: Pentazocine.
Pharmacokinetics
Absorption: Pentazocine has an oral bioavailability is 95%, pre-systemic (first-pass) metabolism accounts for 80% (±10%).
Distribution: Pentazocine has a volume of distribution is 250 - 550 litre. plasma protein binding is 48 - 75 %.
Elimination: it is metabolised via Hepatic, plasma half-life is 2 hr, renal excretion is 10 %.
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Indications
Pentazocine is primarily indicated in conditions like Moderate to severe pain.
Pentazocine is also indicated for secondary conditions like Anesthesia, Mild to moderate dementia in alzheimer's disease, Premedication in anaesthesia.
Contraindications
Pentazocine is contraindicated in conditions like Hypertension, Respiratory depression, Raised intracranial pressure, Opioid dependence, CNS depression, Porphyria, Hypersensitivity.
Dosage
Pentazocine's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 75 mg | 75 mg | Every 4h | IV,IM,SC | Not to exceed 600mg/day. Frequency may be increased upto 8 times if needed. |
| 62.5 mg | 62.5 mg | Every 8h | PO | Frequency may increased to 4 times, if needed. |
| Paediatric Dosage (20kg) | ||||
| No data. | ||||
| Neonatal Dosage (3kg) | ||||
| No data. | ||||
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Pentazocine in overdosage may give rise to further complications which include Pruritis , Epilepsy , Sinus tachycardia , Hypotension , Hypertension , Flushing , Hypoventilation, Tachycardia .
Pentazocine produces potentially life-threatening effects which include Respiratory depression, Agranulocytosis. Careful monitoring is needed with proper medical management.
The signs and symptoms that are produced after acute overdosage of Pentazocine are Increase in BP , Tachycardia , Respiratory depression.
Pentazocine is known to cause more or less tolerable side effects which are usually transient. These include Blurred vision, Chills, Constipation , Cramps , Diplopia, Dizziness, Dyspnea, Euphoria, Fever, Flushing, Hallucination , Headache, Nausea, Nystagmus , Reaction at injection site, Sedation , Sweating , SweatingX, Vivid dreams.
Warnings / Precautions
Available Brands
Storage Conditions
Drug Classification
- 1.2.2 — Opioid analgesics