Levitra

Levitra is a medicine that contributes to the improvement of erectile function.

[1]

Indications of the levitra

It is used to eliminate impotence (the drug is a regulator of potency) - with its presence, a man is not able to achieve the required level of erection for a successful sexual act, and also to preserve it.

[2]

Release form

The release is carried out in tablets with a volume of 10 or 20 mg, in blister packs, 1 or 4 pieces inside them. There is also a dosage of drugs, which is 5 mg - such tablets are produced on 4 pieces inside a blister, 5 such plates inside the box.

[3], [4]

Pharmacodynamics

The most known PDE is the specific form of PDE-5, which participates in cleavage processes by hydrolyzing HMF (this function is one of the options for regulating cGMP indices during penile erection).

Vardenafil is a blocker of PDE-5, and also potentiates the local effect of internal NO, which is secreted through the nerve receptors of cavernous bodies under the influence of a sexual stimulus. The NO element is required to activate the guanilate cyclase enzyme, which increases the level of cGMP and helps to relax the smooth muscles inside the cavernous bodies. As a result, the influx of blood into the penis area increases. In this way, Levitra potentiates the body's natural response to a sexual stimulus.

It was found that the mean values required to slow the PDE5 are 0.7 nM. Therefore, vardenafil is a potent, highly selective inhibitor. The use of 20 mg of vardenafil already after a lapse of 15 minutes causes an erection in some men, which is sufficient for penetration. To get a full reaction, you should wait 25 minutes.

[5]

Pharmacokinetics

Absorption.

Absorption after oral administration is very fast, when used on an empty stomach, the peak LS can be reached after 15 minutes, but often (in 90% of cases) it takes about 1 hour. At reception together with fat food the speed of absorption of a medicine on the average decreases on 20%.

The absolute bioavailability is about 15%. The stationary distribution volume is 208 liters. The indices of the synthesis of the main element (M1) with the protein inside the blood plasma are equal to a maximum of 95% (reversible reaction). After 1.5 hours in the sperm of a healthy male, up to 0.00012% of the dose can be noted.

Metabolic processes and excretion.

Metabolism is mainly carried out with the help of liver enzymes and hemoprotein systems. The average half-life is about 4-5 hours, and in the main product of metabolism (it is formed during the de-ethylation of the piperazine part inside the molecule), it is approximately 4 hours.

Metabolism products are excreted mainly through the digestive tract (about 91-95%), and the remainder through the kidneys.

Changes in AUC and other values of drugs in different categories of patients.

AUC values in the elderly are often increased by 52%.

In people with kidney failure in severe degree, the AUC increases by approximately 21%, and the peak level of drugs decreases by 23%.

As a result of disorders of the hepatic activity, the clearance rates decrease in accordance with the severity of the functional disorder.

[6], [7]

Dosing and administration

The drug is consumed inside, without being tied to food, about 25-60 minutes before sexual intercourse.

The standard mode of use.

The recommended size of the initial portion is 10 mg. The medicine can not be taken more than once in 24 hours. Taking into account the tolerability of the course and the effectiveness of the therapeutic effect, the daily dosage can be increased to 20 mg or reduced to 5 mg.

The use of a therapeutic agent for people with disorders of hepatic activity.

The recommended initial dose of the drug is 5 mg. In the course of treatment, it can be increased to 10 mg.

[10], [11], [12], [13]

Contraindications

The main contraindications:

• the presence of hypersensitivity to any of the elements of the drug;
• persons using drugs containing nitrates or NO donors, and in addition substances that inhibit the activity of CYP3A4 (among such indinavir, itraconazole and ritonavir with clarithromycin, and in addition erythromycin with ketoconazole);
• treatment with other medications for impotence;
• use in men who are banned from sexual activity (for example, if there are background diseases in the CAS area, such as heart failure in the acute phase or unstable angina);
• disorders of hepatic function in the severe stage;
• conducting hemodialysis at the initial stage of renal pathology;
• decreased blood pressure (at a standstill below 90 mm Hg);
• a recent myocardial infarction or stroke (six months before and less);
• degenerative forms of pathologies in the retina that have a hereditary nature (such as retinitis pigmented nature);
• newborn babies and children, as well as women.

Caution is required when appointing in such cases (you need to evaluate the ratio of benefit and risk):

• The anatomical deformation of the penis (this includes a variety of curvatures, and in addition Peyronie's disease and cavernous fibrosis);
• the presence of predisposition to the development of priapism - for example, myeloma, anemia sickle-cell character, the presence of a tendency to bleeding, as well as leukemia;
• ulcer in the stage of exacerbation.

Side effects of the levitra

The use of the drug may cause the following side effects:

• diseases that are of an infectious nature: development of conjunctivitis;
• problems in the work of the central nervous system and the psyche: the occurrence of headaches and sleep disorder;
• impairment of visual function: deterioration of visual acuity and color perception, a feeling of pain or discomfort in the eye area, an increase in IOP, photosensitivity and hyperemia in the conjunctiva;
• disorder of auditory activity: sudden development of deafness, and in addition, ear ringing and vertigo;
• immune lesions: Quincke edema or swelling, which is allergic, as well as allergy symptoms;
• disorders in the work of CCC: the emergence of angina, ventricular tachyarrhythmia, tachycardia, palpitations, the development of vasodilation or myocardial infarction, as well as a decrease in pressure values;
• disorders of the gastrointestinal tract: nausea, gastritis, dry mouth mucosa, dyspeptic symptoms, GERD, vomiting, abdominal pain and diarrhea;
• lesions in the sternum and mediastinum, and in addition respiratory activity: dyspnea, congestion in the region of the nose with paranasal sinuses;
• problems affecting the liver and ZHVP: increased activity of transaminases;
• damage to the subcutaneous layer and skin surface: rashes or erythema;
• disruption of the function of connective tissue, musculature and skeleton: pain in the back area, increased muscle tone, increased values of CK, and also myalgia;
• disorders in the mammary glands and genitals: the development of priapism and increased erection;
• systemic: pain in the sternum and poor health.

[8], [9]

Overdose

When vardenafil is used in a dose of 40 mg twice a day, the patient may develop severe back pain. At the same time, no symptoms of toxic effects on the central nervous system and musculature are noted.

To remove the overdose, it is necessary to carry out the usual supporting procedures. The effectiveness of hemodialysis is very low.

Interactions with other drugs

When combined with drugs that slow the activity of CYP, the vardenafil clearance rate may decrease.

Combination with erythromycin in a daily portion of 1.5 g leads to a fourfold increase in the level of AUC, as well as a triple increase in peak values of the drug (5 mg).

Combined use with ketoconazole in a dose of 0.2 g causes a 10-fold increase in AUC, and in addition a 4-fold increase in peak values of drugs (5 mg), so their dose needs to be adjusted.

Combination of the drug with drugs that slow down the HIV proteases of the active ingredient (indinavir in a daily dosage of 2.4 g) causes a 16-fold increase in the AUC and a 7-fold increase in the peak level of the active Levitra element.

Simultaneous use with ritonavir (the size of the daily portion - 1.2 g) raises 13 times the peak values of the drug at a dosage of 5 mg, and also causes a 49-fold increase in the total value of PPC per day. In addition, the half-life of vardenafil is significantly prolonged (approximately 26 hours).

When combined with NO donors and nitrates, their effect is intensified, but this interaction does not develop if the 24-hour interval between uses is observed.

The use of excessively large portions of vardenafil in combination with sodium nitroprusside results in a slight increase in antiaggregant effect.

It is necessary to observe the time intervals between the use of the drug and α-blockers, and also apply them exclusively at a stable level of blood pressure. For example, for use with terazosin it is necessary to withstand a 6-hour period.

[14]

Storage conditions

Levitra should be kept in a closed place from small children and the penetration of moisture place. The temperature level is a maximum of + 30 ° C.

[15], [16],

Shelf life

Levitra can be used for 3 years after the release of the therapeutic agent.

Analogues

Analogues of the medication are preparations of Viagra, Adamax, and also Genagra.

[17], [18]

Reviews

Levitra is considered effective and at the same time an affordable medicine that helps to improve an erection. Patients leave positive comments about the drug, noting that it can be consumed together with alcoholic beverages, as well as in the presence of certain diseases affecting CAS.