Lorazepam 1 mg

Active substance:

Content

Pharmacological group

Composition and release form

in blister pack of 14; in a box of 1, 2 or 7 blisters.

in blister pack of 14; in a box of 1, 2 or 7 blisters.

in blister pack of 14; in a box of 1, 2 or 7 blisters.

Description of the dosage form

Round, biconvex, film-coated tablets:

with a dosage of 0.2 mg – pale pink color, labeled “0.2” on the one hand;

with a dosage of 0.3 mg – pale red, labeled “0.3” on one side;

with a dosage of 0.4 mg – dull red, labeled “0.4” on one side.

On the cross section, two layers are visible.

pharmachologic effect

Pharmacodynamics

Selectively interacting with imidazolin I1 receptors located in the brain stem, reduces sympathetic activity.

Moxonidine has a high affinity for imidazoline I1 receptors and only slightly binds to central alpha2-adrenergic receptors due to the interaction with which dry mouth and sedation are explained.

Reduces insulin resistance of tissues.

Effect on hemodynamics: a decrease in systolic and diastolic blood pressure with a single and prolonged administration of moxonidine is associated with a decrease in the pressor action of the sympathetic system on peripheral vessels, a decrease in peripheral vascular resistance, while cardiac output and heart rate do not change significantly.

Pharmacokinetics

Absorption – 90%. Cmax in plasma (after taking a pill containing 0.2 mg of moxonidine) is 1.4–3 ng / ml and is reached after 60 minutes. Bioavailability – 88% (food intake does not affect the pharmacokinetics).

Distribution volume – 1.4–3 l / kg. Gets through the BBB. Plasma protein binding – 7.2%.

Major metabolites: 4,5-dihydromoxonidine and guanidine derivatives.

Lorazepam 1 mg

T1 / 2 moxonidine and metabolites is 2.5 and 5 h, respectively. Within 24 hours, more than 90% of moxonidine is excreted by the kidneys, approximately 78% unchanged and 13% as a dehydrogenated derivative. Less than 1% is excreted in the feces. Does not accumulate with prolonged use.

Pharmacokinetics in the elderly

Lorazepam 1 mg

Age-related changes in pharmacokinetics are observed, probably related to slightly higher bioavailability and / or reduced metabolic activity. However, these changes are not clinically significant.

Pharmacokinetics for renal failure

Moxonidine clearance largely correlates with creatinine clearance. In patients with moderate renal insufficiency (Cl of creatinine in the range of 30–60 ml / min) equilibrium plasma concentrations and final T1 / 2 are approximately 2 and 1.5 times higher than in patients with arterial hypertension with normal kidney function (Cl creatinine >90 ml / min). In patients with severe renal insufficiency (creatinine Cl

Contraindications

hypersensitivity to the drug;

sick sinus syndrome, severe bradycardia;

age up to 18 years (efficacy and safety have not been established).

severe chronic renal failure and severe liver failure (due to lack of experience with the application);

Use during pregnancy and lactation

There are no clinical data on the negative impact on the course of pregnancy. However, care should be taken when prescribing Physiotens ® to pregnant women. During the period of treatment it is recommended to stop breastfeeding,

Side effects

From the side of the central nervous system: dizziness, headache, drowsiness, sleep disturbance.

Since the cardiovascular system: excessive reduction of blood pressure, orthostatic hypotension.

On the part of the digestive tract: dry mouth, nausea.

From the skin and subcutaneous adipose tissue: skin rash, itching, angioedema.

These symptoms usually gradually decrease during the first weeks of treatment.

Interaction

Perhaps combined use with thiazide diuretics, ACE inhibitors and slow calcium channel blockers. There is a mutual reinforcement of action when used together with these and other antihypertensive drugs.

There is no pharmacokinetic interaction with hydrochlorothiazide (perhaps combined use), glibenclamide (glyburide), digoxin. Tricyclic antidepressants can reduce the effectiveness of centrally acting antihypertensive drugs (co-administration is not recommended). Moderately enhances reduced cognitive ability in patients taking lorazepam. Enhances the sedative effect of benzodiazepines. There is no pharmacodynamic interaction when co-administered with moclobemide.

Dosage and administration

Inside, regardless of the meal, the initial dose (in most cases) – 0.2 mg per day; the maximum daily dose is 0.6 mg (divided into 2 doses); maximum single dose – 0.4 mg;

in renal insufficiency (Cl creatinine 30–60 ml / min) and in patients on hemodialysis, a single dose is 0.2 mg, the maximum daily dose is 0.4 mg.

Overdose

Symptoms: headache, sedation, drowsiness, excessive decrease in blood pressure, dizziness, general weakness, bradycardia, dry mouth, vomiting, fatigue and pain in the stomach. Potentially possible short-term increase in blood pressure, tachycardia, hyperglycemia.

Treatment: alpha adrenoreceptor antagonists can reduce or eliminate paradoxical hypertension. In case of hypotension, the restoration of BCC is recommended due to the introduction of fluid and the introduction of dopamine. Bradycardia can be stopped by atropine. There is no specific antidote.

special instructions

If it is necessary to cancel simultaneously taken beta-blockers and Physiotensa, first cancel beta-blockers and only a few days later – Physiotens ®. During treatment requires regular monitoring of blood pressure, heart rate, ECG. Discontinue physiotherapy should be gradually. Patients with a rare hereditary pathology of galactose intolerance, lactase deficiency or glucose-galactose malabsorption should not take this drug.

There are no data on the adverse effect of moxonidine on the ability to drive a car and to control machines and mechanisms. There are reports of drowsiness and dizziness during treatment with moxonidine. This should be considered when performing the above actions.

Manufacturer

Solvay Pharmaceuticals GmbH, Germany.

Storage conditions of the drug Physiotens ®

Keep out of the reach of children.

Expiration date of the drug Physiotens ®

film coated tablets

film coated tablets

Do not use after the expiration date printed on the package.

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