MINIMS PHENYLEPHRINE HYDROCHLORIDE EYE DROPS 10% W/V FOR OPHTHALMIC USE

Product Information

Registration Status: Active

MINIMS PHENYLEPHRINE HYDROCHLORIDE EYE DROPS 10% W/V is approved to be sold in Singapore with effective from 1990-04-20. It is marketed by BAUSCH & LOMB (SINGAPORE) PTE LTD, with the registration number of SIN04319P.

This product contains Phenylephrine 10% w/v in the form of SOLUTION. It is approved for OPHTHALMIC use.

This product is manufactured by LABORATOIRE CHAUVIN SA in FRANCE.

It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Description

Phenylephrine is a sympathomimetic amine that acts predominantly on α-adrenergic receptors. It is mainly used to treat nasal congestion, but may also be useful in treating hypotension and shock, hypotension during spinal anaesthesia, prolongation of spinal anaesthesia, paroxysmal supraventricular tachycardia, symptomatic relief of external or internal hemorrhoids, and to increase blood pressure as an aid in the diagnosis of heart murmurs.

Indication

Phenylephrine is mainly used to treat nasal congestion, but may also be useful in treating hypotension and shock, hypotension during spinal anaesthesia, prolongation of spinal anaesthesia, paroxysmal supraventricular tachycardia, symptomatic relief of external or internal hemorrhoids, and to increase blood pressure as an aid in the diagnosis of heart murmurs.

Mechanism of Action

In general, α₁-adrenergic receptors mediate contraction and hypertrophic growth of smooth muscle cells. α₁-receptors are 7-transmembrane domain receptors coupled to G proteins, G_q/11. Three α₁-receptor subtypes, which share approximately 75% homology in their transmembrane domains, have been identified: α_1A (chromosome 8), α_1B (chromosome 5), and α_1D (chromosome 20). Phenylephrine appears to act similarly on all three receptor subtypes. All three receptor subtypes appear to be involved in maintaining vascular tone. The α_1A-receptor maintains basal vascular tone while the α_1B-receptor mediates the vasocontrictory effects of exogenous α₁-agonists. Activation of the α₁-receptor activates G_q-proteins, which results in intracellular stimulation of phospholipases C, A₂, and D. This results in mobilization of Ca²⁺ from intracellular stores, activation of mitogen-activated kinase and PI₃ kinase pathways and subsequent vasoconstriction. Phenylephrine produces its local and systemic actions by acting on α₁-adrenergic receptors peripheral vascular smooth muscle. Stimulation of the α₁-adrenergic receptors results in contraction arteriolar smooth muscle in the periphery. Phenylephrine decreases nasal congestion by acting on α₁-adrenergic receptors in the arterioles of the nasal mucosa to produce constriction; this leads to decreased edema and increased drainage of the sinus cavities.

Pharmacokinetics

Absorption: Completely absorbed after oral administration. It has a reduced bioavailability (compared to pseudoephedrine) following oral administration due to significant first-pass metabolism in the intestinal wall. Compared to IV administration, bioavailability is approximately 38%. Peak serum concentrations are achieved approximately 0.75-2 hours following oral administration. Phenylephrine should be administered parenterally to achieve cardiovascular effects. Occasionally, systemic effects are observed following oral inhalation.
Distribution
Metabolism: Undergoes extensive first-pass metabolism in the intestinal wall and extensive metabolism in the liver. Sulfate conjugation, primarily in the intestinal wall, and oxidative metabolism by monoamine oxidase (MAO) represent the principle routes of metabolism. Glucuronidation occurs to a lesser extent. Phenylephrine and its metabolites are mainly excreted in urine/ .
Elimination

Active Ingredient/Synonyms

Source of information: Drugbank (External Link). Last updated on: 3^rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.