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Composition:


active ingredient: yohimbine hydrochloride;


1 tablet contains yohimbine hydrochloride 5 mg;


excipients: potato starch; lactose, monohydrate; calcium stearate; hypromellose; coelactose (a mixture of lactose, monohydrate, and powdered cellulose (75:25)).


Dosage form. Pills.


Basic physical and chemical properties: tablets of white or white with a yellowish tinge of color, with a chamfer.


Pharmacotherapeutic group. Remedies used for erectile dysfunction. Yohimbine. ATX code G04B E04.


Pharmacological properties.


Pharmacodynamics.


Yohimbine Hydrochloride is a potency enhancing drug (aphrodisiac), an alkaloid from the bark of the West African tree Corynanthe.


The mechanism of action is due to selective blocking of α2-adrenergic receptors. Increases the central exchange of adrenaline, that is, activates adrenergic neurons in the central nervous system, which causes a psychostimulating effect and increases the response. In addition, it may affect the serotonergic, dopaminergic and cholinergic transmission systems of nerve impulses.


It has been experimentally established that yohimbine activates sexual behavior and normalizes sexual activity and the ability to coitus reduced due to stress, restores erectile dysfunction caused by activation of alpha-adrenergic receptors.


The therapeutic effect in humans is largely due to the effects of yohimbine on the central nervous system. In addition, a possible mechanism of action is the expansion of penile vessels and a direct effect on the tissues involved in erection.


An explanation for the frequent delays in the appearance of the effect for 2-3 weeks may be the accumulation of the active metabolite 11-hydroxyohimbine.


Pharmacokinetics.


Suction. Yohimbine is completely absorbed in the digestive tract within 1 hour. Cmax in the blood is reached in 45-75 minutes. AUC (area under the plasma concentration curve) as a bioavailability parameter shows pronounced fluctuations. This is not due to incomplete absorption from the gastrointestinal tract, but to the effect of the first passage through the liver. Cmax and AUC depend on the dose. When the drug is administered orally at the recommended doses, accumulation of the drug does not occur.


Distribution. It is evenly distributed in fabrics. In blood plasma, 82% of yohimbine binds to protein. Only a small part of yohimbine and the active metabolite 11-hydroxyohimbine (approximately 2% of the plasma concentration) penetrates the intercellular fluid.


Metabolism. Yohimbine is metabolized by the liver and extrahepatic. Two hydroxylated metabolites were identified: the active metabolite 11-hydroxyohimbine and the less active metabolite 10-hydroxyohimbine.


Output. The Half-Life of yohimbine after a single dose is from 0.25 to 2.5 hours. The Half-Life of 11 – hydroxyohimbine is longer-approximately 6 hours. After repeated use, yohimbine is eliminated in the time range from less than 1 hour to more than 8 hours.


Clinical characteristics.


Indications.


Erectile dysfunction of various origins.


Contraindications.


Hypersensitivity to any components of the drug. Severe hypotension. The presence of severe liver and Kidney Diseases, Treatment with adrenomimetics.


Interactions with other drugs and other types of interactions.


Concomitant administration of clonidine is not indicated, since the effects of the drugs are mutually neutralized; a sharp decrease in blood pressure is also possible. Yohimbine can alter the activity of antihypertensive agents (calcium antagonists, beta-blockers, angiotensin-converting enzyme inhibitors). Yohimbine may potentiate the effect of antidepressants and increase the risk of their side effects, may reduce the activity of tranquilizers, in particular alprazolam – do not use yohimbine together with these drugs. Clomipramine increases the level of yohimbine in blood plasma. When used simultaneously with adrenomimetics (epinephrine, norepinephrine, mezaton, fetanol, ephedrine), their effectiveness may decrease, and in rare cases, the hypertensive effect may increase.


Application features. Caution should be exercised when prescribing the drug to patients with arterial hypertension, heart diseases (coronary heart disease, tachyarrhythmias), peptic ulcer of the stomach and duodenum, impaired kidney or liver function, mental illnesses with affective symptoms or anxiety, glaucoma.

Do not use in elderly patients.


It is not recommended to use the drug in cases of danger of a sudden decrease in blood pressure with reflex tachycardia.


The drug contains lactose, so if the patient is found to be intolerant to certain sugars, you should consult your doctor before taking this medicine.


Use during pregnancy or lactation.


The drug is not intended for use in women.


Ability to influence the reaction rate when driving vehicles or other mechanisms.


Given that patients with increased individual sensitivity may experience adverse reactions (dizziness, tremor) when using the drug, while taking the drug, you should refrain from driving vehicles and other work that requires concentration of attention.


Dosage and administration.


Prescribe to adults inside, with meals, without chewing and with a glass of water.


The recommended dose is 1-2 tablets 1-3 times a day.


The dose should be selected individually, starting with taking 2.5 mg of yohimbine 3 times a day and gradually increasing the dose to a maximum of 1-2 tablets (5-10 mg) 3 times a day.


If it is necessary to take yohimbine in a single dose of 2.5 mg, the drug should be used with the possibility of such a dosage.


The effect often occurs 2-3 weeks late. In case of side effects, a dose reduction is recommended. After the side effects disappear, the dose can be gradually increased.


The duration of treatment depends on the severity of the disease and is 3-4 weeks.


Children. Do not use in children.


Overdose.


Symptoms of intoxication. Approximately 20-30 minutes after oral administration of an excessive dose, general weakness, generalized paresthesia, memory and coordination disorders, severe headache, dizziness, tremor, tachycardia, arterial hypertension, a feeling of fear and anxiety, a significant increase in the level of norepinephrine in blood plasma (normally 150-550 pg/ml), nausea, vomiting, mydriasis, salivation and lacrimation, increased sweating occur. After about 4 hours, chest pain occurs, which can last for several hours. Headache, hypertension, and tachycardia may also persist for several hours.


Treatment. Withdrawal of the drug. In the early stages-gastric lavage, followed by the use of Activated Carbon and sodium sulfate (Glauber's salt) or only activated carbon.


As an antidote for overdose, clonidine can be used, which quickly neutralizes both mental effects and effects from the sympathetic nervous system. The initial dose of clonidine is 0.1-0.2 mg orally. Next, it is necessary to take several separate doses of 0.1 mg at intervals of 1 hour until normalization of cardiovascular activity and reduction of other symptoms.


For the treatment of hypertensive crisis, beta-blockers can be used in combination with an alpha-blocker (for example, phentolamine) or a peripheral vasodilator (for example, nitroprusside). If you feel fear, anxiety, or hallucinations, you can prescribe benzodiazepines if sympathomimetic reactions are absent or poorly expressed. Do not prescribe phenothiazine-type neuroleptics.


Adverse reactions.


Cardiac disorders: increased heart rate.


Neurological disorders: headache, dizziness, sleep disorders, nervousness, tremor, increased agitation, increased anxiety, mania, sweating.


Gastrointestinal disorders: rarely-nausea and vomiting, loss of appetite, diarrhea.


Changes in the skin and subcutaneous tissue: redness of the skin.


Vascular disorders: increased blood pressure.


Others: decreased diuresis, priapism (a pathological condition characterized by the occurrence of a prolonged erection that is not associated with sexual arousal); people with increased individual sensitivity may have allergic reactions (including bronchospasm, lupus-like syndrome, angioedema).

Tags: Yohimbine