Product Information
Registration Status: ActiveSIN06718P
CYCLOMYDRIL STERILE OPHTHALMIC SOLUTION is approved to be sold in Singapore with effective from 1991-09-12. It is marketed by ALCON PTE LTD, with the registration number of SIN06718P.
This product contains Cyclopentolate 0.2%, and Phenylephrine 1% in the form of SOLUTION. It is approved for OPHTHALMIC use.
This product is manufactured by ALCON LABORATORIES INC in UNITED STATES.
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.
Product Reference
Important Note: For generic product, the SPC/PIL provided may not be brand specific.
{{/items}} {{^items}}Description
A parasympatholytic anticholinergic used solely to obtain mydriasis or cycloplegia. [PubChem]
Indication
Used mainly to produce mydriasis and cycloplegia for diagnostic purposes.
Mechanism of Action
By blocking muscarinic receptors, cyclopentolate produces dilatation of the pupil (mydriasis) and prevents the eye from accommodating for near vision (cycloplegia).
Pharmacokinetics
- Absorption
- Absorbed following ophthalmic administration.
- Distribution
- Metabolism
- Elimination
Toxicity
Oral LD50 in the rat is 4000 mg/kg and 960 mg/kg in the mouse. Symptoms of overdose include tachycardia, dizziness, dry mouth, behavioral disturbances, uncoordination and drowsiness.
Active Ingredient/Synonyms
(+-)-Cyclopentolate | (±)-cyclopentolate | 1-Hydroxy-alpha-phenylcyclopentaneacetic acid 2-(dimethylamino)ethyl ester | 2-(dimethylamino)Ethyl 1-hydroxy-alpha-phenylcyclopentaneacetate | 2-(dimethylamino)Ethyl 2-(1-hydroxycyclopentyl)-2-phenylacetate | 2-Phenyl-2-(1-hydroxycyclopentyl)ethanoic acid beta-(dimethylamino)ethyl ester | alpha-(1-Hydroxycyclopentyl)benzeneacetic acid 2-(dimethylamino)ethyl ester | beta-(dimethylamino)Ethyl (1-hydroxycyclopentyl)phenylacetate | beta-Dimethylaminoethyl (1-hydroxycyclopentyl)phenylacetate | Ciclopentolato | Cyclopentolate | Cyclopentolatum | α-(1-hydroxycyclopentyl)benzeneacetic acid 2-(dimethylamino)ethyl ester | β-dimethylaminoethyl (1-hydroxycyclopentyl)phenylacetate | Cyclopentolate |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.
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, Gq/11. Three α1-receptor subtypes, which share approximately 75% homology in their transmembrane domains, have been identified: α1A (chromosome 8), α1B (chromosome 5), and α1D (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 α1A-receptor maintains basal vascular tone while the α1B-receptor mediates the vasocontrictory effects of exogenous α1-agonists. Activation of the α1-receptor activates Gq-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
(-)-m-Hydroxy-alpha-(methylaminomethyl)benzyl alcohol | (-)-m-Hydroxy-α-(methylaminomethyl)benzyl alcohol | Benzenemethanol, 3-hydroxy-.alpha.-[(methylamino)methyl]-, (R)- | Benzenemethanol, 3-hydroxy-alpha-((methylamino)methyl)-, (R)- | Benzyl alcohol, m-hydroxy-alpha-((methylamino)methyl)-, (-)- | Fenilefrina | l-(3-Hydroxyphenyl)-N-methylethanolamine | Phenylephrine | Phenylephrinum | R(-)-Phenylephrine | Phenylephrine |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.