PETHIDINE

Pethidine is derived from phenylpiperidine and is an opioid analgesic. It acts primarily as a mu-receptor agonist. Like most opioid analgesics, it mimics endoenous opioids through activating opioid receptors in the central and peripheral nervous system. It reduces the release of neurotransmitters and in addition reduces the activities of postsynaptic neurons within the spinal wire thus preventing transmission of the pain impulse.

Uses

Pethidine hydrochloride is used as an analgesic for the treatment of moderate to severe pain including pain after childbirth, and pain before, during and after a surgical operation. It is used to relieve moderate to severe pain. Customarily, this drug is used to relieve pain in various circumstances.

Warnings

Pethidine should be used with caution in:

Breathing difficulties
Newborn babies
Premature babies
Elderly patients
Debilitated patients
Severe liver disease
Severe kidney disease
Biliary tract disorders
Underactive thyroid gland
Adrenocortical insufficiency
Shock
Enlarged prostate gland
Rapid or erratic heartbeat
Myasthenia gravis (a condition which causes muscles weakness)
Acute alcoholism
Convulsive disorders (fits)
Severe continuing pain
Cor pulmonale (a heart problem after long-term lung disease)

It should not be used in:

History of allergies to pethidine
Coma
Raised intracranial pressure (increased pressure on the brain)
Patients with head injuries
A tumour on your adrenal gland called a phaeochromocytoma,
Respiratory depression or obstructive airways disease
Patients receiving monoamine oxidase inhibitors or within two weeks following their withdrawal

Side Effects

Pethidine may have the following side effects:

Hypotension
Fatigue
Drowsiness
Dizziness
Nervousness
Headache
Restlessness
Malaise
Confusion
Depression
Hallucinations
Tremors
Muscle twitches
Increased intracranial pressure
Seizure
Serotonin syndrome
Rash
Urticaria
Nausea
Vomiting
Constipation
Anorexia
Stomach cramps
Xerostomia
Biliary spasm
Paralytic ileus
Sphincter of Oddi spasm
Ureteral spasms
Decreased urination
Pain at injection site
Weakness
Dyspnoea
Histamine release
Physical and psychological dependence

Precautions

Precautions

Pethidine may impair your ability to drive or operate machinery.

Take extra caution in people with the following conditions:

Hypovolaemia
Cardiovascular disease
Adrenal insufficiency
Biliary tract disorder
CNS depression or coma
History of drug abuse or acute alcoholism
Head injury
Intracranial lesions
Elevated intracranial pressure
Hepatic or renal impairment
Morbidly obese
Prostatic hyperplasia
Toxic psychoses
Pre-existing respiratory compromise (hypoxia and/or hypercapnia)
COPD or other obstructive airway disease
Sickle-cell disease
Supraventricular tachycardia
Thyroid dysfunction
Elderly and debilitated patients
Pregnancy (avoid prolonged use or high doses at term) and lactation.

Interactions

Pethidine can interact with the following

Aciclovir
Cimetidine
Ritonavir
Phenytoin
Barbiturates
Alcohol
Benzodiazepines
Phenothiazines
TCAs
Other CNS depressants

There is an increased risk of serotonin syndrome with MAOIs (not be given concurrently or within 14 days of their discontinuation), serotonin agonists, serotonin reuptake inhibitors, sibutramine, TCAs.

Overdose & Brands

Symptoms of overdose include the following:

CNS/respiratory depression
Mydriasis,
Bradycardia
Pulmonary oedema
Chronic tremor
CNS excitability
Seizures

Available Brand:

Demerol