Zovicrem Lipstick 50 Mg/G Cream 1 Tube 2 G With Dosing Pump

Zovicrem Lip (Acyclovir) 50 Mg / G Cream 1 Tube 2 G (With Dosing Pump)

ACTION AND MECHANISM

- Antiviral. Acyclovir is a virostatic with a structure similar to guanosine, which inhibits cellular synthesis of viral DNA.

Antiviral action is manifested only in viruses in replication phase. This selective action is due to the fact that in its first phosphorylation to acyclovir monophosphate, an enzyme of the virus, thymidine kinase, intervenes, an enzyme for which acyclovir shows 200 times more affinity than for the human enzyme. In cells not infected with the virus, this first phosphorylation is very slow. Subsequent phosphorylations until the active form of the drug, acyclovir triphosphate, is carried out using cellular enzymes.

Acyclovir triphosphate is capable of inhibiting viral replication in three ways:

* Selective inhibition of viral DNA polymerase.

* Competition between acyclovir triphosphate with guanosine triphosphate for incorporation into viral DNA.

* Interruption of the chain when incorporated into the viral DNA.

It is especially active against herpes simplex virus (HSV) types 1 and 2, and the varicella zoster virus. In descending order, it also shows in vitro activity against Epstein-Barr virus (EBV), human herpes virus type 6 (HHV-6) and cytomegalovirus (CMV). Compared to CMV (virus without thymidine kinase), its activity is much less than that of famciclovir or foscarnet.

PHARMACOKINETICS

Topical route:

- Absorption: acyclovir hardly crosses the intact skin, reaching undetectable levels (<0.01 mcg / ml) after its administration 4 times a day for 7 days. In the skin of people with herpes zoster cp of 0.01-0.28 mcg / ml is reached.

- Distribution: low plasma protein binding (9-33%). Its Vd is 0.8 l / kg.

- Metabolism: it undergoes partial metabolism due to hydroxylation and oxidation reactions. 2 metabolites, 8-hydroxy-acyclovir and 9-carboxymethoxy-methyl-guanine, both inactive, have been described.

Enzyme inducing / inhibiting capacity : does not appear to have significant effects.

- Elimination: mainly in urine in unchanged form. After topical administration, 0.02-9.4% of the urine dose is recovered unchanged. Its CLr is 173-353 ml / min / 1.73 m2 and t1 / 2 2.5-3.3 h.

Pharmacokinetics in special situations :

- Renal impairment: an increase in cp has been observed, with values ​​of 0.78 mcg / ml. However, due to its minimal topical absorption this does not seem likely to be significant.

- Other situations: there are no data available about how the age or degree of liver function could affect the pharmacokinetics of acyclovir after topical administration.

INDICATIONS

Lip:
- Treatment of symptoms of [HERPES SIMPLE LABIAL], such as itching, stinging or tingling.

POSOLOGY

- Adults: apply a thin layer on the lesions 5 times a day, approximately every 4 h, omitting the application during the hours of sleep at night. To achieve maximum effectiveness, it is important to start treatment as soon as possible, as soon as the first symptoms appear.

- Children and adolescents <18 years: no dosage adjustment is required. Perform under medical supervision.

- Elderly: no dosage adjustment is required.

Treatment duration: 5 days. If complete healing has not occurred, extend 5 more days to a total of 10 days. If symptoms worsen or do not improve during this period, reevaluate the diagnosis.

Missed dose: administer the next dose at the usual time. Do not double the next dose.

POSOLOGY IN KIDNEY FAILURE

No specific dosage recommendations have been made.

POSOLOGY IN LIVER FAILURE

No specific dosage recommendations have been made.

RULES FOR THE CORRECT ADMINISTRATION

Wash your hands before and after applying the medicine, as well as avoid rubbing lip lesions with your hands or towels as much as possible, so that the infection does not worsen or spread to other parts of the body or to other people, since it is a contagious process.

CONTRAINDICATIONS

- Hypersensitivity to acyclovir, valacyclovir or any other component of the medicine.

PRECAUTIONS

- [IMMUNODEFICIENCY]. In severely immunosuppressed patients, such as in [HIV INFECTION] or patients undergoing [TRANSPLANT], the use of topical acyclovir may be insufficient to combat the infection. The use of oral acyclovir should be considered.

ADVICE TO THE PATIENT

- Treatment should start as soon as possible after the onset of symptoms.

- Acyclovir does not prevent transmission of the virus. Therefore, precautions should be taken to reduce the risk of possible contagion, such as avoiding contact of injuries with hands or other objects.

- Check with your doctor if symptoms worsen or do not improve after using acyclovir for 10 days.

- Avoid applying it on eyes or mucosa.

SPECIAL WARNINGS

- Treatment should start as soon as the first symptoms appear.

- Patients with severe infection, severe immunosuppression, or frequent recurrences, may require oral acyclovir for infection control.

- It is recommended to make a differential diagnosis in young children in case of a possible first herpes infection, since the symptoms could be confused with other oral or teething disorders.

INTERACTIONS

They have not been described. It is unlikely due to its minimal absorption.

PREGNANCY

Animal safety : No harmful effects have been observed in pregnancy, embryo-fetal development, delivery or postnatal development.

Safety in humans : Adequate and well-controlled studies in humans are not available. There are very limited data on the use in pregnant women, where no side effects have been observed in the fetus. Its administration is only accepted if there are no safer therapeutic alternatives, and the benefits outweigh the possible risks.

Effects on fertility : No specific human studies have been conducted topically. Its systemic administration did not negatively affect the sperm (morphology, mobility, count).

LACTATION

Animal safety: no data available.

Safety in humans: acyclovir is excreted in milk. After the administration of 200 mg 5 times a day, concentrations in milk were obtained 0.6-4.1 times the maternal cp, which would mean a dose for the infant of 0.3 mg / kg / 24 h. However, it is estimated that due to its poor skin absorption the levels in milk would be minimal. Its administration is only accepted if there are no safer therapeutic alternatives, and the benefits for the mother outweigh the possible risks in the infant.

CHILDREN

No specific problems have been described in children that require a readjustment. It is recommended to use under medical recommendation, especially in <12 years.

Cold sores are a recurrence of an infection inside the mouth that usually contracts at an early age. It is recommended to make a first medical diagnosis in children, since the symptoms of the first infection could go unnoticed or be confused with disorders of the teeth or other oral processes.

ELDERLY

No specific problems have been described in the elderly that require a dosage adjustment.

EFFECTS ON DRIVING

It does not appear to have a significant effect.

ADVERSE REACTIONS

Adverse reactions are described according to each frequency interval, being considered very frequent (> 10%), frequent (1-10%), infrequent (0.1-1%), rare (0.01-0.1%) , very rare (<0.01%) or of unknown frequency (cannot be estimated from the available data).

- Dermatological: infrequent local reactions in the area of ​​application, such as a local burning sensation, [ITCHING], [SKIN DRYNESS], [SKIN DESCAMATION]; rare [Erythema], [CONTACT DERMATITIS].

- Allergic: very rare [HYPER-SENSITIVITY REACTIONS], including [ANGIOEDEMA].

ADVERSE REACTIONS RELATED TO EXCIPIENTS

- Because it contains cetostearyl alcohol, it can cause local skin reactions, such as [CONTACT DERMATITIS].

- This medicine contains propylene glycol, so it can cause [SKIN IRRITATION].

OVERDOSE

Symptoms: significant poisoning is unlikely due to its route of administration. After accidental intake of 10 g of cream (500 mg of acyclovir), no symptoms have been described. There have been cases of patients who received up to 20 g orally, without presenting symptoms.

Measures to take:

- Antidote: there is no specific antidote.

- General measures of elimination: although it does not seem necessary to take any measures, acyclovir is eliminated by hemodialysis.

- Monitoring: clinical status of the patient.

- Treatment: symptomatic.

Zovicrem Lipstick Leaflet 50 Mg / G Cream 1 Tube 2 G With Metering Pump