Betamethasone + Phenylephrine + Lignocaine
Indications
This preparation rectal ointment is indicated for relief of the symptoms of-
- itching,
- irritation,
- discomfort or pain associated with local non-infective anal or
- peri-anal conditions such as external hemorrhoids.
Composition
The composition of this rectal ointment is given below:
- Betamethasone (as 17 valerate) 0.05%
- Phenylephrine hydrochloride 0.1%
- Lignocaine hydrochloride 2.5%
Pharmacology
Betamethasone is a corticosteroid with mainly glucocorticoid activity. It induces phospholipase A2 inhibitory lipase (lipocortins) and sequentially inhibits the release of arachidonic acid, thereby depressing the formation, release, and activity of prostaglandins, leukotrienes, and other inflammatory mediators.
Phenylephrine is a sympathomimetic with mainly direct effects on alpha-adrenergic receptors and weak beta-adrenergic activity. It causes vasoconstriction of the arterioles of the nasal mucosa and conjunctiva; activates the dilator muscle of the pupil to cause contraction; produces vasoconstriction of arterioles in the body and produces systemic arterial vasoconstriction.
Lidocaine alters signal conduction in neurons by blocking the fast voltage-gated Na+ channels in the neuronal cell membrane responsible for signal propagation. With sufficient blockage, the membrane of the postsynaptic neuron will not depolarize and will thus fail to transmit an action potential.
Phenylephrine is a sympathomimetic with mainly direct effects on alpha-adrenergic receptors and weak beta-adrenergic activity. It causes vasoconstriction of the arterioles of the nasal mucosa and conjunctiva; activates the dilator muscle of the pupil to cause contraction; produces vasoconstriction of arterioles in the body and produces systemic arterial vasoconstriction.
Lidocaine alters signal conduction in neurons by blocking the fast voltage-gated Na+ channels in the neuronal cell membrane responsible for signal propagation. With sufficient blockage, the membrane of the postsynaptic neuron will not depolarize and will thus fail to transmit an action potential.
Dosage & Administration
A course of treatment should be limited to 7 days. Apply a small amount of ointment two or three times a day initially, using the applicator if internal administration is required. When inflammation is subsiding, once-daily application is sufficient in most cases. Or as directed by the physician.
Contraindications
Primary cutaneous viral infections (e. g. herpes simplex, chickenpox). Hypersensitivity to any components of the drug. The use of this ointment is not indicated in the treatment of primarily infected skin lesions caused by infection with fungi (e. g. candidiasis, tinea); or bacteria (e. g. impetigo).
Side Effects
Signs of hypersensitivity may appear. Prolonged and intensive treatment with highly active corticosteroid preparations may cause local atrophic changes in the skin.
Pregnancy & Lactation
There is inadequate evidence of safety in human pregnancy.
Precautions & Warnings
Long-term continuous therapy should be avoided where possible, particularly in infants and children, as adrenal suppression can occur.
Therapeutic Class
4-Quinolone preparations, Phlebotonic & Vascular protecting preparation
Storage Conditions
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.