Instruction for use: Pipofezine

Latin name of substance Pipofezine

Pipofezinum (genus. Pipofezini)

Chemical name

5-Methyl-3- (4-methyl-1-piperazinyl) -5H-pyridazino [3,4b] [1,4] benzoxazine (as hydrochloride)

Gross formula

C₁₆H₁₉N₅O

Pharmacological group:

Antidepressant

The nosological classification (ICD-10)

F32 Depressive episode: Adynamic subdepression; Astheno-adynamic subdepressive states; Asthenoadressive disorder; Astheno-depressive disorder; Asthenodepressive state; Astheno-depressive state; Major Depressive Disorder; Vyaloapatichesky depression with retardation; Double Depression; Depressive pseudodement; Depressive illness; Depressive mood disorder; Depressive disorder; Depressive mood disorder; Depressive state; Depressive disorders; Depressive syndrome; Depressive syndrome larviated; Depressive syndrome in psychoses; Depressed masks; Depression; Depression Depletion; Depression with the phenomena of inhibition within the framework of cyclothymia; Depression is smiling; Involutional depression; Involutionary melancholy; Involutional depression; Manic-depressive disorder; Masked Depression; Melancholic Attack; Neurotic depression; Neurotic depression; Shallow Depression; Organic depression; Organic depressive syndrome; Simple depression; Simple melancholic syndrome; Psychogenic depression; Reactive depression; Reactive depression with moderate psychopathological symptoms; Reactive depressive states; Reactive depression; Recurrent depression; Seasonal depressive syndrome; Severostatic depression; Senile Depression; Symptomatic Depression; Somatogenic depression; Cyclotymic depression; Exogenous depression; Endogenous depression; Endogenous Depressive Conditions; Endogenous Depression; Endogenous depressive syndrome

F33 Recurrent depressive disorder: Major depressive disorder; Secondary depression; Double Depression; Depressive pseudodement; Depressive mood disorder; Depressive disorder; Depressive mood disorder; Depressive state; Depressive syndrome; Depressed masks; Depression; Depression is smiling; Involutional depression; Involutional depression; Masked Depression; Melancholic Attack; Reactive depression; Reactive depression with moderate psychopathological symptoms; Reactive depressive states; Exogenous depression; Endogenous depression; Endogenous Depressive Conditions; Endogenous Depression; Endogenous depressive syndrome

CAS code

24886-52-0

Characteristics of the substance Pipofezine

Crystalline powder is greenish-yellow in color. Easily soluble in water, practically insoluble in ethanol, chloroform.

Pharmacology

Pharmacological action - antidepressive, timoleptic, sedative.

Indiscriminately inhibits the reverse neuronal capture of serotonin and norepinephrine from the synaptic cleft, which leads to an increase in their concentrations in the postsynaptic receptor region and relief of symptoms of depression. Virtually does not possess cholinolytic activity and does not affect the activity of MAO.

After oral administration, it is quickly and completely absorbed from the digestive tract. Bioavailability is about 80%. Cmax in the blood is reached after 2 hours. Binding to plasma proteins is about 90%. Undergoes biotransformation in the liver with the formation of inactive metabolites. T1 / 2 - 16 hours Excreted mainly by the kidneys.

The modified release dosage form provides a gradual release of the pipophasin in the digestive tract. The released pypofezin quickly and almost completely absorbed into the digestive tract. An in vitro study showed that pipophezin is not a substratum of cytochrome P450 isoenzymes CYP2C9, CYP2C19, CYP2D6 and CYP3A4, but is mainly metabolized by CYP1A2. With a single oral application of the modified release tablet (150 mg) Cmax of pipophezin in the blood is achieved after 3-4 hours.

Application of the substance Pipofezine

Depressive disorders of mild and moderate severity (including depressive states in chronic somatic diseases).

Contraindications

Hypersensitivity, hepatic and / or renal failure, concurrent administration of MAO inhibitors, pregnancy, breast-feeding.

Restrictions on the use

Chronic heart failure, myocardial infarction, ischemic heart disease, condition after acute impairment of cerebral circulation, severe infectious diseases, diabetes, children's age (there is no information on the safety of use in children).

Application in pregnancy and lactation

The FDA action category is not defined.

Side effects of the substance Pipofezin

Headache, dizziness, nausea, vomiting, allergic reactions.

Interaction

Potentsiruet effects of alcohol and other drugs, depressing the central nervous system, antihistamines. Reduces the effectiveness of anticonvulsant therapy.

An in vitro study showed that pipiphezin is not an inhibitor or inducer of cytochrome P450 isoenzymes CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4, so it is unlikely that it interacts with drugs that are substrates of these isoenzymes.

Routes of administration

Inside.