Pharmacological properties  testosterone propionate 100mg – selective beta 1-blocker, without its own sympathomimetic activity, has no membrane stabilizing action. As with other beta1-adrenergic blockers, the mechanism of action in hypertension is unclear. However, it is known that testosterone propionate 100mg reduces renin activity in plasma reduces myocardial oxygen demand, slows the heart rate (HR). Has antihypertensive, antiarrhythmic and antianginal effects. Blocking in low doses of beta 1-adrenergic receptors of the heart, reduces the formation of catecholamines stimulated cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP), decreases the intracellular current calcium ions, inhibits all functions of the heart, reduces the atrioventricular (AV) conduction and excitability. If you exceed the therapeutic dose has beta2-adrenoceptor blocking action. Total peripheral vascular resistance at the beginning of the drug in the first 24 hours, is increased (as a result of reciprocal increase in the activity of alpha-adrenoceptor stimulation and removal of beta2-adrenoceptor), after 1-3 days returned to the initial value, and long-term use – is reduced. Antihypertensive effect associated with decreased cardiac output, sympathetic stimulation of peripheral vascular disease, decreased activity sympathoadrenal system (SAS) (important for patients with initial hypersecretion renin) sensitivity reduction in response to the decrease in blood pressure (BP) and the influence on the central nervous system ( CNS). When hypertension effect develops after 2-5 days, stable operation is noted after 1-2 months. Antianginal effect is due to a decrease in myocardial oxygen demand by reducing contractility and other functions of the myocardium, lengthening diastole, improving myocardial perfusion. By increasing the end-diastolic left ventricular pressure and increase the tension of muscle fibers of the ventricles can be increased oxygen demand, especially in patients with chronic heart failure (CHF). When used in high therapeutic doses, unlike non-selective beta-blocker, has a less pronounced the effect on the organs containing beta2-adrenergic receptors (pancreas, skeletal muscle, smooth muscle of the peripheral arteries, bronchi and uterus) and carbohydrate metabolism; It does not cause a delay of sodium ions in the body; severity atherogenic action different from the action of propranolol. Pharmacokinetics testosterone propionate 100mg almost completely absorbed in the gastrointestinal tract, food intake does not affect absorption. The effect of “first pass” through the liver, is small, resulting in a high bioavailability (90%). testosterone propionate 100mg metabolized by oxidative way without subsequent conjugation. All metabolites have a strong polarity and the kidneys. Major metabolites detected in plasma and urine did not exhibit pharmacological activity. Data obtained from experiments with microsomes in vitro human liver demonstrate that testosterone propionate 100mg is metabolized mainly via isoenzyme CYP3A4 (about 95%) and CYP2D6 isozyme plays only a small role. Communication with the plasma proteins around 30%. Distribution Volume – 3.5 l / kg. The total clearance – about 15 l / h. The maximum plasma concentration is determined after 2-3 hours. Permeability through the blood brain barrier and the placental barrier – is low. The half-life of plasma (10-12 hours) have provided efficiency within 24 hours after receiving a single daily dose. testosterone propionate 100mg excreted two paths, 50% of the dose is metabolized in the liver to inactive metabolites . About 98% is excreted by the kidneys, of which 50% is excreted as unchanged; less than 2% -. through the intestine (in the bile) Since elimination takes place in the kidneys and liver alike, patients with impaired liver function or renal insufficiency correction dose is not required. The pharmacokinetics of testosterone propionate 100mg is linear and independent of age. In patients with chronic heart failure testosterone propionate 100mg plasma concentrations above and half-life is longer compared with healthy volunteers.
Indications
- Arterial hypertension;
- Coronary heart disease: prevention of attacks of stable angina.
Contraindications
- Hypersensitivity to the drug and other beta-blockers;
- congestive heart failure and chronic heart failure decompensation requiring of inotropic therapy;
- cardiogenic shock;
- collapse;
- atrioventricular (AV) block II-III degree, without a pacemaker;
- sinoatrial block;
- sick sinus syndrome;
- bradycardia (heart rate before treatment of less than 60 beats / min.);
- severe hypotension (systolic blood pressure less than 100 mmHg)
- cardiomegaly (without heart failure);
- severe bronchial asthma and chronic obstructive pulmonary disease (COPD) history;
- The expressed disturbances of peripheral circulation;
- Reynaud’s syndrome;
- metabolic acidosis;
- pheochromocytoma (without the simultaneous use of alpha-blockers);
- simultaneous reception of monoamine oxidase inhibitors (MAOIs) (except MAO-B inhibitors);
- concomitant use floctafenine and sultopride.
- age of 18 years (effectiveness and safety have been established).
The caution
psoriasis, depression (including history), diabetes mellitus (may mask the symptoms of hypoglycemia), allergic reactions (in history), bronchospasm (in history), conducting desensitizing therapy, Prinzmetal angina, AV block I degree, expressed disturbances renal function (creatinine clearance (CC) of less than 20 ml / min); expressed human liver; thyrotoxicosis, advanced age.
Pregnancy and lactation Pregnancy testosterone propionate 100mg has no direct cytotoxic, mutagenic and teratogenic effects, but has pharmacological effects that may cause harmful effects on pregnancy and / or the fetus or newborn. Typically, beta-blockers reduce placental perfusion, which leads to a slowing of fetal growth, fetal death, miscarriage or premature birth. In the fetus and newborn child may have abnormal reactions such as fetal developmental delay, hypoglycemia, bradycardia. testosterone propionate 100mg -Teva should not be used during pregnancy, the use is possible in the case if the benefit to the mother outweighs the risk of side effects in the fetus and / or child. In the case where treatment with testosterone propionate 100mg -Teva regarded as necessary, should monitor blood flow in the placenta and uterus, and also to observe the growth and development of the child and in the event of adverse events in respect of pregnancy and / or fetal take alternative therapy. It is necessary to carefully examine the newborn after delivery. Symptoms of hypoglycaemia and bradycardia are generally occur within the first 3 days of life. Breastfeeding Period Data on the penetration of testosterone propionate 100mg into breast milk is not. Therefore, the drug testosterone propionate 100mg -Teva not recommended for women during lactation. If necessary, use during lactation, breast-feeding should be discontinued.
Dosing and Administration
The drug testosterone propionate 100mg -Teva taken orally on an empty stomach in the morning, 1 time per day with a little liquid, in the morning before breakfast, during or after it. Tablets should not be chewed or triturate.
In all cases of reception mode and selects the physician dose for each patient individually, in particular, given the patient’s heart rate and condition. When hypertension and coronary heart disease the drug is prescribed 5 mg 1 time per day. If necessary to increase the dose of 10 mg 1 time per day. In the treatment of hypertension and angina pectoris the maximum daily dose is 20 mg 1 time / day.
For patients with severe renal function impairment (creatinine clearance less than 20 ml / min.) Or severe liver problems, the maximum daily dose is – 10 mg 1 time per day . Increasing the dose in such patients should be carried out with extreme caution. No dose adjustment in elderly patients is not required.
Side effects:
The frequency of adverse reactions listed below was determined according to the following (World Health Organization): very often – at least 10%; often – at least 1% but less than 10%; infrequently – at least 0.1% but less than 1%; rare – less than 0.01% but less than 0.1%; very rarely – less than 0.01%, including isolated reports. From the heart and blood vessels: very often – slowing of heart rate (bradycardia, particularly in patients with CHF); palpitations, often – marked reduction of blood pressure (especially in patients with CHF), a manifestation of vasoconstriction (increased peripheral circulatory disorders, feeling of cold in the extremities (paraesthesia); rarely – a violation of AV conduction (until the development of a complete transverse blockade and heart failure), arrhythmia , orthostatic hypotension, worsening of heart failure with the current development of peripheral edema (swelling of the ankles, feet, shortness of breath), chest pain. from the nervous system: often – dizziness, headache, asthenia, fatigue, sleep disturbances, depression, anxiety, rarely -sputannost consciousness or short-term memory loss, “nightmarish” dream, hallucination, myasthenia gravis, tremor, muscle cramps usually these effects are mild and are usually within 1-2 weeks after starting treatment.. From the sensory organs: rarely – visual disturbances, reduced lacrimation (to consider when wearing contact lenses), tinnitus, hearing loss, ear pain is very rare – dryness and soreness of the eyes, conjunctivitis, taste disturbances. The respiratory system: rarely – bronchospasm in patients with bronchial asthma or obstructive airways disease; rarely – allergic rhinitis; nasal congestion. From the digestive system: often – nausea, vomiting, diarrhea, constipation, dryness of the oral mucosa, stomach pain; rarely – hepatitis, increased activity of liver enzymes (alanine aminotransferase, aspartate aminotransferase), increasing the concentration of bilirubin, a change of taste. From the musculoskeletal system: rarely – arthralgia, back pain.From the urogenital system: very rarely – a violation of potency, the weakening of the libido. Laboratory findings: rarely – increased concentration of triglycerides in the blood; in some cases – thrombocytopenia, agranulocytosis, leukopenia. Allergic reactions: rarely – itching, rash, hives For the skin: rarely – increased sweating, flushing of the skin, rash, psoriasiform skin reactions; very rare – alopecia, beta-blockers may exacerbate psoriasis. Other: a syndrome of “cancellation” (increased frequency of angina attacks, increased blood pressure).
Overdose symptoms: arrhythmia, ventricular premature beats, bradycardia, AV block, marked reduction in blood pressure, congestive heart failure, hypoglycemia, akrotsianoz, shortness of breath, bronchospasm, dizziness, fainting, seizures. Treatment: In case of overdose occur, you’ll first need to stop taking the drug, to gastric lavage, appoint adsorbing means to spend symptomatic therapy. In severe bradycardia – intravenous administration of atropine. If the effect is insufficient, you can enter with caution agent with positive chronotropic effect. Sometimes it may require temporary staging an artificial pacemaker. In marked decrease in blood pressure – intravenous plasma-solutions and vasopressors. When hypoglycemia can be shown intravenous glucagon or intravenous dextrose (glucose). If AV blockade: patients should be under constant surveillance, and receive treatment of beta-adrenergic agonists such as epinephrine. If necessary – setting an artificial pacemaker. When exacerbation of heart failure – intravenous diuretics, drugs with positive inotropic effects and vasodilators. When bronchospasm – appointment of bronchodilators, including beta2-agonists and / or aminophylline.
Interaction with other drugs
on the efficacy and tolerability of drugs can affect the simultaneous use of other drugs. Such interaction may also occur when the two drugs taken after a short time. The doctor should be informed about the use of other drugs, even if the application is carried out without a prescription.
Class I antiarrhythmics (eg, quinidine, disopyramide, lidocaine, phenytoin; flecainide, propafenone), while the use of testosterone propionate 100mg may reduce AV conduction and myocardial contractility.
Antiaritmicheksie means class III (eg, amiodarone) may increase the violation of AV conduction.
The action of beta-blockers for topical application (eg eye drops for glaucoma treatment) may enhance the systemic effects of testosterone propionate 100mg (lowering blood pressure, slowing of the heart rate).
parasympathomimetics while the use of testosterone propionate 100mg may strengthen the AV conduction and increase the risk of bradycardia. Simultaneous use of the drug testosterone propionate 100mg -Teva with beta-adrenergic agonists (e.g., isoprenaline, dobutamine) may reduce the effect of both preparations.
The combination of testosterone propionate 100mg with agonists affecting beta- and alpha-adrenergic receptors (such as norepinephrine, epinephrine), may enhance the effects of vasoconstrictor these funds arising from the participation of the alpha-adrenergic receptors, resulting in increased blood pressure. Such interactions are more likely when using non-selective beta-blockers. Mefloquine while the use of testosterone propionate 100mg may increase the risk of bradycardia.
The allergens used for immunotherapy, or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving testosterone propionate 100mg. Iodosoderzhaschie radiopaque diagnostic agents for intravenous administration increases the risk of anaphylactic reactions. Phenytoin intravenous administration, the means for inhalation anesthesia (derivatives of hydrocarbons) increase the intensity of cardiodepressive action and the likelihood of blood pressure lowering.
The effectiveness of insulin and hypoglycemic agents for oral administration may change the treatment with testosterone propionate 100mg (masking the symptoms of developing hypoglycemia: tachycardia, increased blood pressure).
The clearance of lidocaine and xanthine (except theophylline) may be reduced due to the possible increase of their plasma concentrations, especially in patients with initially increased clearance of theophylline under the influence of smoking. Antihypertensive effect of weakening nonsteroidal anti-inflammatory drugs (NSAIDs) (delay sodium and kidney of prostaglandin synthesis blockade), corticosteroids, and estrogens (delay of sodium ions). Cardiac glycosides, methyldopa, reserpine and guanfacine blockers “slow” calcium channel blockers (verapamil, diltiazem), amiodarone and other antiarrhythmic drugs increase the risk of developing or worsening of bradycardia, AV block, cardiac arrest and heart failure. Nifedipine can lead to a significant reduction in blood pressure. Diuretics, clonidine, sympatholytic, hydralazine and other antihypertensive drugs may lead to an excessive reduction in blood pressure.
The action of non-depolarizing muscle relaxants and anticoagulant effect of coumarin during the treatment period may be extended testosterone propionate 100mg th. Tricyclic and tetracyclic antidepressants, antipsychotics (neuroleptics), ethanol, sedatives and hypnotics increase central nervous system depression.
Not recommended simultaneous application with MAO inhibitors due to the significant increase in the hypotensive action. Break in treatment between receiving MAO inhibitors and testosterone propionate 100mg must not be less than 14 days. Non-hydrogenated ergot alkaloids increase the risk of peripheral circulatory disorders.
Ergotamine increases the risk of peripheral circulatory disorders. Sulfasalazine increases the concentration of testosterone propionate 100mg in blood plasma. Rifampicin shortens the half-life of testosterone propionate 100mg.
Cautions
monitoring the condition of patients taking the drug testosterone propionate 100mg -Teva should include measurement of blood pressure and heart rate, ECG conduct, determining the concentration of blood glucose in patients with diabetes mellitus (1 every 4-5 months.). In elderly patients it is recommended to monitor renal function (1 time in 4-5 months.).
It is necessary to train the patient’s heart rate calculation method and instruct on the need of medical advice in heart rate less than 50 beats / min.
Before treatment, it is recommended to carry out research in respiratory function patients with a history of bronchopulmonary history.
patients who use contact lenses, you should consider that in the context of drug treatment may decrease the production of tear fluid.
Using the drug -Teva testosterone propionate 100mg in patients with pheochromocytoma have a risk of paradoxical hypertension (if not previously reached effective alpha blockade adrenoceptor).
When testosterone propionate 100mg thyrotoxicosis may mask certain clinical signs of hyperthyroidism (eg, tachycardia). Abrupt withdrawal of the drug in patients with thyrotoxicosis is contraindicated because the symptoms can increase.
In diabetes may mask tachycardia caused by hypoglycemia. In contrast, nonselective beta-blockers practically no increase insulin-induced hypoglycemia and delay recovery of the concentration of glucose in the blood to normal.
With the simultaneous use of clonidine its reception can be terminated only a few days after discontinuation of testosterone propionate 100mg -Teva. Perhaps the increased severity of hypersensitivity reactions and the lack of effect of conventional doses of epinephrine with aggravated allergic history.
In the case of the need for a planned surgical treatment drug should be discontinued 48 hours before general anesthesia. If the patient has taken the drug before surgery, he should choose the drug for general anesthesia with minimal negative inotropic effect.
Reciprocal activation of the vagus nerve can be eliminated by intravenous administration of atropine (1-2 mg).
Drugs that deplete the depot of catecholamines (including h. . reserpine), may enhance the effect of beta-blockers, so patients taking such drug combinations should be under constant medical supervision in order to identify pronounced reduction in blood pressure and bradycardia.
patients with bronhospasticheskimi diseases can be prescribed with care cardioselective beta-blockers in the case of intolerance and / or ineffectiveness of other antihypertensives. While taking beta-blockers in patients with concomitant asthma may be exacerbated airway resistance. Exceeding the dose of testosterone propionate 100mg -Teva in these patients there is a risk of bronchospasm. In case of patients increasing bradycardia (heart rate less than 50 bpm. / Min.), Marked reduction of blood pressure (systolic blood pressure less than 100 mm Hg), AV blockade, it is necessary to reduce the dose or discontinue treatment.It is recommended to discontinue therapy with testosterone propionate 100mg -Teva in the development of depression.
Do not abruptly discontinue the treatment because of the risk of severe arrhythmias and myocardial infarction. Abolition of the drug was gradually reducing the dose for 2 weeks or more (reduce dose by 25% in 3-4 days).
It is necessary to cancel prior to the study drug concentration in the blood and urine catecholamines, Normetanephrine, vanilinmindalnoy acid, antinuclear antibody titers. Smokers efficiency beta-blockers lower. Effects on ability to drive and operate machinery which requires high concentration use of the drug testosterone propionate 100mg -Teva does not affect the ability to drive vehicles according to a study in patients with CAD. However, the ability to drive vehicles or operate technically complex mechanisms may be impaired as a result of individual reactions. It should be emphasized at the start of treatment, after changing the dose and while consuming alcohol. anabolic steroids online pharmacy
