Promethazine ampoules

Promethazine Promethazine

Indications for use of promethazine

Promethazine is used for the symptomatic treatment of allergies such as hay fever, urticaria, immediate treatment of anaphylactic reactions, treatment of nausea, dizziness, labyrinthine disorders, travel sickness, and anesthesia.

Mechanism of action of promethazine

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Phenothiazine derivatives
Blocking postsynaptic dopamine receptors in the mesolimbic pathway of the brain
Strong blocker of alpha adrenergic receptors in the brain
Decreased release of pituitary and hypothalamic hormones
– Competitive histamine H1 receptor antagonist
Muscarinic receptor blocker; With this mechanism, it causes anti-nausea effects and reduces stimulation of the reticular system of the brainstem.

Pharmacokinetics of promethazine

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Absorption: fast and complete.
Its significant hepatic first passage reduces bioavailability.
Bioavailability:
Oral 25%, anal 23.4-21.7%
Start of effect:
Oral, anal, intramuscular: 20 minutes, intravenous: 5 minutes
Effect length: 4-4 hours (up to 12 hours)
Serum courier:
Oral syrup 2.8 hours, anal 8.2 hours
Protein binding: 93%
metabolism:
Hepatic (hydroxylation by CYP2D6 and N demethylation by CYP2B6, significant first hepatic passage)
half life:
Suppositories and syrups 19-16 hours
Muscular 10 hours
Intravenous 16-9 hours
Excretion: urine and feces