Azaphen (Pipofezine) tablets - Instructions for Use, Dosage, Side Effects, Reviews

Synonyms: Azaphen

Active substance: Pipofezine.

ATC - N06AX Other antidepressants.

Pharmacological group - Antidepressants.

Pipofezine (Azafen or Azaphen) is a tricyclic antidepressant (TCA) approved in Russia for the treatment of depression. It was introduced in the late 1960s and is still used today.

Pipofezine has been shown to act as a potent inhibitor of the reuptake of serotonin. In addition to its antidepressant action, pipofezine has sedative effects as well, suggesting antihistamine activity. Other properties such as anticholinergic or antiadrenergic actions are less clear but are likely.

Azaphen (Pipofezine) tablets Variations

Azaphen (Pipofezine) tablets 25 mg, N50

Azaphen (Pipofezine) tablets 25 mg, N250

Azaphen (Pipofezine) MR (prolong) tablets 150 mg, N30

Nosological classification (ICD–10)

F06 Other mental disorders due to damage and dysfunction of the brain or somatic disease;

F32 Depressive episode.

Azaphen (Pipofezine) Composition, structure and packing

Azaphen: The tablets are yellowish-green color, Valium, chamfered; tolerance of marbling.

Other ingredients: potato starch, colloidal silicon dioxide (Aerosil), microcrystalline cellulose, lactose, povidone (polyvinylpyrrolidone low molecular medical), magnesium stearate.

Azaphen MR: The modified-release tablets are yellowish-green color, round, biconvex; tolerance of marbling.

Excipients: Hypromellose (Methocel K4M Premium), Kollidon 25 (povidone), microcrystalline cellulose, colloidal silicon dioxide (Aerosil), talc (magnesium silicate), magnesium stearate.

Pharmacological action

Tricyclic antidepressant. Blocking neuronal monoamine uptake presynaptic membranes increases their content in the synaptic cleft leading to reduction of symptoms of depression. Timoleptic effect of the drug is combined with a sedative and anxiolytic activity effect. Unlike tricyclic antidepressants possesses anticholinergic properties which are not affected by the activity of MAO has not cardiotoxicity.

Pharmacokinetics

Absorption

Rapidly and completely absorbed from the gastrointestinal tract. Bioavailability - about 80%. T max after administration of tablets - 2 hours.

In tablets Azaphen MR active substance is contained in a special matrix-supported, sustained release of pipofezine in the digestive tract. Pipofezin liberated rapidly and almost completely absorbed from the gastrointestinal tract. When a single oral tablet Azafen MV 150 mg C max pipofezine blood achieved in 3–4 hours and is 111 ng / ml.

Distribution and metabolism

Binding to plasma proteins - 90%.

Largely biotransformation in the liver to form inactive metabolites.

In an in vitro study shows that is not a substrate pipofezine isoenzymes CYP2C9, CYP2C19, CYP2D6 and CYP3A4, and is metabolized mainly influenced by CYP1A2.

Excretion

T 1/2 after taking the pills - 16 h, T 1/2 after a dose modified-release - 9 hours. Eliminated from the body primarily by the kidneys.

The residence time of the drug in the organism (MRT) - average 13.4 hours (10 to 20 hours). Repeated receptions fluctuations drug concentration in blood plasma in the gap between the two doses are smoothed. Eliminated from the body primarily by the kidneys.

Azaphen (Pipofezine) Dosage

The initial dose for adults is 25–50 mg in 2 divided doses (morning and afternoon). With good endurance gradually increase the dose to 150–200 mg/day (3–4 hours, last admission at bedtime), in some cases - up to 400 mg/day. The optimal daily dose - 150–200 mg, the maximum daily dose - 400–500 mg. When the desired effect of switching to maintenance dose - 25–75 mg/day. The course of treatment - up to 1 year (at least 1–1.5 months).

After establishing the optimal daily dose using tablets Azaphen 25 mg, administered Azafen MB (modified-release tablets) 150 mg of 1 times (morning) or 2 times (morning and evening) based on efficacy and tolerance.

Azaphen (Pipofezine) Overdose

Data about overdose are not available.

Azaphen (Pipofezine) Drug Interactions

With simultaneous application Azaphen potentiates the effects of ethanol and other CNS depressants, antihistamines and anticoagulants.

Reduces the effectiveness of anticonvulsant therapy.

In an in vitro study demonstrated that pipofezine not an inhibitor or inducer of isozymes CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4, it is unlikely Azaphen drug interaction with drugs that are substrates of these isoenzymes. Fluvoxamine, propafenone, mexiletine, ciprofloxacin, as inhibitors of CYP1A2, pipofezine can increase the concentration in plasma.

Pregnancy and lactation

The drug is contraindicated during pregnancy and lactation.

Azaphen (Pipofezine) Side effects

CNS: headache, dizziness.

From the digestive system: nausea, vomiting.

Other: allergic reactions.

Indications

Depressive disorders mild to moderate severity (including depression with chronic medical conditions).

Contraindications

Severe hepatic and/or renal failure;

Concomitant use of monoamine oxidase inhibitors;

Pregnancy;

Lactation (breastfeeding);

Hypersensitivity to the drug.

Precautions should be prescribed the drug for chronic heart failure, myocardial infarction, with ischemic heart disease, condition after acute stroke, infectious diseases, diabetes, childhood (insufficient data on the safety of use).

Cautions

After the transfer to MAO inhibitor therapy on Azaphen should be an interval of 2 weeks.

A periodic monitoring of liver and kidney.

During treatment, the use of alcohol is prohibited.

Effects on ability to drive vehicles and management mechanisms

During treatment, patients should refrain from activities potentially hazardous activities that require attention and quickness of psychomotor reactions, such as driving.

Azaphen (Pipofezine) Reviews

Always I felt that the depression I had never been, so when my doctor prescribed the drug "Azafen" I was surprised. Why would I? I got to the hospital with symptoms of "prolonged muscle pain ...". The drug I saw cut with other appointments. Discharged in satisfactory condition. Recommendations for follow-up treatment "Azaphen" I left ...
And now the house carefully review the instructions, I periodically return to " Azaphen ". It is easy antidepressant, but still try not to sit down and get used to the pills.
It does not satisfy me, and the internal discomfort with itself, some leading out of a sense of balance, inability to concentrate on the right, and so on. N. States is reminiscent of the " Azaphen ".
The recommended course of treatment (which is 1-1.5 months) do not use. One tablet of Azaphen helps improve internal spirit.
Recommend reception " Azaphen " Of course I will not, after all, need to consult a doctor. But it is not necessary to be afraid of this drug. In my opinion, and for me personally, this is the most harmless, it helps to relieve mild depression medication.

Great Drug

Antidepressant " Azaphen " I took prescribed by a doctor, quite a long time, about half a year. Cardinally improve their condition, I have not noticed. As it has been depressive mood, and left. But sleep got up, becoming a deep and calm. And at times reduced life does not give me rest increased anxiety.

Special side-effects are not noticed. Is that the first time that has just started taking this drug, periodically suffered from headaches.

So I can say that "Azaphen " - antidepressant light not strong, both in terms of side effects and therapeutic effect. But personally, I like it.

Strong Nerve

You can not do without the sedative tablets. After all, modern life and its pace is not allowed to live in peace for most people. Nothing can be done have to resort to sedatives and antidepressants. But for a man like me, my character is not sugar and because of this, neither I nor others have to oh how hard times. I can yell at someone, maybe it's good shout all stresses are faster, but then I start to torture yourself, they say why I did it. Therefore, insomnia and poor appetite, and other symptoms of depression are not rare guests at me. But my anxiety and fear that something do not give off too and I happen sometimes protracted depression. Among the anti-depressants I was taking pills Azaphen, one of the last and effective. They are 25 mg (in multiples of 250 pieces), small, round, whitish. I bought a package for 342 rubles, not cheap, in my opinion a little expensive. Every human body reacts to these drugs individually, one suit, the other way around. For me pills " Azaphen " went better than others, although there are side effects from them. I observed after a dose and slight dizziness and drowsiness. But the main thing Azaphen with neyrofulolom (so the doctor advised me) helped me get rid of depression, phobias and all disappeared.
He took pills for two weeks, three tablets a day, you can extend the course for another two weeks, in this case, the treatment effect will be more stable and long-lasting. I'm after a course of Azaphen became, if not the iron, the more calm for sure. Cheerful (life has become happier), too, and in this I see the main effect of taking Azaphen tablets worthy of an antidepressant, and recommend to you!

" Azaphen " - Wonder drug with the help of which I began to live, not exist!
Last year, I went through a lot of stress. Tell us briefly (being pregnant), my sister gave birth to the COP could not recover for a long time, lying in gynecology child we took, after the ill-law. Insidious disease of the 20th century-oncology. she gave birth to a son was a crybaby, took care of her mother in law, m there and started every day in my head there was only one question and if I get sick, 2 weeks buried in-law, then I fell into a tough depression. parents took the child. I lost weight on every day from 72 kg I lost weight to 58 kg. has not yet reached lo good neurologist and he told me it is a miracle drug prescribed Azaphen to these pills, I only existed since the early days as the beginning of taking these pills, I began to live a new life. and so grateful to the neurologist and the manufacturers of these pills. Side effects I have not noticed, but I will say one pill brought me back to life!