PROKTALEK [Phenylephrine hydrochloride + Lidocaine] 2.5 + 50 mg Cream for external use
instructions for the medical use of
the medicinal product
PROKTALEK
Tradename:
Proktalek, Прокталек
International non-proprietary name
or generic name:
Phenylephrine, Lidocaine; Фенилэфрин, Лидокаин
Composition per
1 g of cream:
active substances: phenylephrine
hydrochloride 2.5 mg, lidocaine 50 mg;
excipients: Glycerin,
white petrolatum, cetyl alcohol, stearyl alcohol, mono- and diglyceride, light
liquid paraffin, methylparaben, propylparaben, propylene glycol, citric acid
monohydrate, disodium edetate, polysorbate 80, aloe, vitamin E, dexpanthenol,
purified water.
Dosage form:
Cream for external use.
Pharmacotherapeutic group:
Drugs for local anesthesia in
proctology.
Code АТХ: N01BB52
Pharmacological
properties
Pharmacodynamics
Phenylephrine is an α-adrenergic agonist with a local vasoconstrictor
effect, which helps reduce exudation, tissue swelling, and itching in the
anorectal area.
Lidocaine is a local anesthetic. Its analgesic and
antipruritic effects are achieved by inhibiting the formation and conduction of
nerve impulses along afferent nerve fibers through depolarization of sodium
channels.
Pharmacokinetics
Phenylephrine undergoes systemic absorption after topical
administration.
The absorption and bioavailability of
lidocaine after rectal administration of cream is approximately 30%. The
half-life is 1-2 hours. Lidocaine is metabolized by oxidative N-dealkylation,
hydrolysis of the amide bond, and hydroxylation of the aromatic ring to form
4-hydroxy-2,6-xylidine, which is the major metabolite. 70% of the drug is
excreted in the urine as this metabolite.
Indications for use
As a symptomatic remedy (pain, itching, burning) for
hemorrhoids, anal fissures, anal itching.
Contraindications
Hypersensitivity to any of the
drug's components, mucosal damage, children and adolescents under 18 years of
age.
Use with caution in patients
with arterial hypertension, hyperthyroidism, diabetes mellitus, thromboembolic
disease, and granulocytopenia.
Method of administration
and dosage
Topically, rectally, after
performing perianal hygiene procedures.
Squeeze a small amount of
cream (about the size of a pea) onto your finger and apply it to the skin
around the anus and into the anal canal to a depth of 1 cm. To overcome
sphincter resistance, apply the cream with your fingertip.
The recommended dose is
twice daily (morning and evening) until symptoms improve, after which the dose
can be reduced. The duration of therapy is determined by your doctor.
Special instructions and precautions
Consult a doctor before using this
medication.
If irritation, bleeding, worsening
of the condition occurs, or if there is no effect within 7 days, discontinue
use and consult a doctor.
Do not use concomitantly with
antihypertensive medications or MAO inhibitors.
Use with caution in elderly
patients, who may be more sensitive to the systemic effects of lidocaine.
Use during pregnancy and breastfeeding
There is insufficient experience with the use of
this drug during pregnancy.
It may be used in pregnant and breastfeeding
women as prescribed by a physician if the potential benefit to the mother
outweighs the potential risk to the fetus and child.
Interaction with other medicinal products
Due to the phenylephrine content,
the effect of antihypertensive medications is reduced. Hypertensive crisis may
occur when co-administered with MAO inhibitor antidepressants.
When using other local anesthetics
and structurally similar agents, the risk of increased systemic effects with
high doses of lidocaine should be considered. Caution should be exercised when
co-administering lidocaine with antiarrhythmic medications. Drugs that reduce
lidocaine clearance (e.g., cimetidine or beta-blockers) may cause potentially
toxic plasma concentrations with repeated high doses of lidocaine over a
prolonged period.
Side effect
Allergic reactions, irritation similar to contact
dermatitis at the application site,
anxiety, tremors, insomnia, nervousness, dizziness,
numbness of the tongue and around the mouth, absentmindedness, irritation,
peripheral vasodilation due to hypertension, arrhythmia, and exacerbation of hyperthyroidism.
If any of the side effects listed in the instructions
worsen, or you notice any other side effects not listed in the instructions,
notify your doctor.
Overdose
No cases of overdose have been reported.
Storage conditions
Store in a dark place at a temperature not exceeding
30°C.
Keep out of reach of children.
Shelf life
3 years. Do not use after the expiration date printed
on the package.
Vacation conditions
Over the counter.
Release form
30g of cream in an aluminum tube with a polypropylene lid. One tube with instructions for use in a cardboard box.