Last Updated on February 19, 2017 by Dr.Derek Fhisher
Most popular brand: Sinequan
Active ingredient: Doxepin
Available dosage forms: 10, 25, 75 mg
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Doxepin general information
An overdose of doxepin could be fatal. Don’t use doxepin when you have used a MAO inhibitor within the previous 14 days. Sertraline might cause other side outcomes. Low-dose doxepin doesn’t appear to be affected by other drugs which affect the cytochrome P450 system. Rather, Rozerem has a solid affinity for particular Melatonin Receptors referred to as MT1 and MT2. Cimetidine may help determine the absorption of doxepin.
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Don’t stop taking sertraline without speaking to your doctor. If it happens to you personally, stop taking doxepin and speak with your doctor. Your physician will have to monitor your progress at regular visits throughout the time you are using doxepin. Just Take the missed dose when you remember it. Keep taking doxepin even should you feel well.
Silenor tablets might cause you to do things when you are still asleep that you can not don’t forget the next morning, like driving an automobile, having sex, or eating food. It can take several weeks or longer that you feel the entire effect of doxepin. Due to this, doxepin should not be taken in conjunction with MAO inhibitors. The following stage is always to demonstrate protease resistance of the new OP-PrP complex.
Should you be not able to receive a complete night’s sleep, don’t take Silenor. It might not work too, or it may cause you to get sleepy the following day. You need to be aware that sertraline may cause you to get drowsy. Don’t stop taking doxepin without speaking to your doctor. Don’t take Silenor if you’re currently taking anMAO Inhibitor. Yes, it’s a greater dose and is technically” only qualified for depression at this strength, but it might work for you as well as save plenty of money.
Take doxepin completely as directed. Keep taking sertraline even should you feel well. Simply Take the missed dose when you remember. Don’t use doxepin when you have taken a MAO inhibitor within the previous 14 days. Pick out the tablet half a hour before going to bed. To find out more on Lunesta, CLICK HERE.
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pharmacodynamics. Doxepin belongs to the tricyclic antidepressants. The antidepressant effect combined with anxiolytic and sedative.
Doxepin inhibits the reuptake of biogenic amines (norepinephrine and serotonin) in the synaptic structures. Also has antihistamine, holinoliticheskie and α 1 – adrenoceptor blocking action. It does not cause euphoria, agitation. .
Pharmacokinetics Doxepin is well absorbed in the gastrointestinal tract, fast (2 – 4 hours after administration) up C max in the blood plasma. Sustained therapeutic concentration in the blood is reached after 2 weeks after the start of treatment.
Doxepin is metabolised in the liver mainly by demethylation with the formation of the major metabolite ; desmetildoksepina (nordoksepin). Binding of doxepin and its metabolites in blood plasma proteins is approximately 76%. The volume of distribution ; about 20 l / kg of body weight. T ½ doxepin is 8 – 24 h, the main active metabolite ; 33 –. 80 hours Doxepin passes through the placenta and the blood-brain barrier and passes into breast milk.
neurotic disorders with symptoms of depression or anxiety. Organic neuroses associated with insomnia. Depressive and anxiety disorders in alcoholism. Depression and anxiety associated with somatic disorders and diseases.
Depression, accompanied by fear and anxiety on the background of psychosis, including involutional depression and the depressive phase of bipolar disorder.
is taken orally. Dose picked individually, depending on the severity of the symptoms and the therapeutic effect
Dose Doxepin is 30 –. 300 mg / day. The dose up to 100 mg may be used singly or divided. Dosages above 100 mg, 3 to be used in reception. The maximum single dose of ; 100 mg (applied before bedtime). For moderate or severe symptoms, the usual initial dose is 75 mg / day. In most patients, this dose is effective. In severe forms of the disease to increase the dose of 300 mg (3 doses) per day.
Patients with insomnia total dose should be distributed so as to apply a higher dose in the evening. In case of insomnia reported as adverse reactions, this scheme can be used as reception or the dose should be reduced.
After achieving a satisfactory therapeutic effect, the dose should be ‘corrected to the minimum maintenance.
The decrease in the severity of anxiety symptoms while taking doxepin is achieved before the antidepressant effect. The antidepressant effect is manifested through 2 – 3 weeks of treatment
Elderly patients with mild symptoms of the disease is recommended half the usual recommended dose of doxepin hydrochloride. (10 – 50 mg daily). Satisfactory clinical effects were obtained after application of doxepin at 30 – 50 mg / day. The dose should be adjusted individually depending on the patient’s clinical response.
Patients with impaired hepatic function should be reduced dose.
hypersensitivity to the drug, cross-sensitivity to other dibenzoksepinam. Mania; severe liver function; glaucoma; urinary retention; concurrent use with MAO inhibitors or the use of up to 2 weeks before treatment doxepin. Hypersensitivity to the tricyclic antidepressants. The tendency to urinary retention.
Doxepin is generally well tolerated. Most side effects of moderate severity occur at the beginning of treatment and disappear after discontinuation of the drug or reducing its dose. Some of the side effects listed below are not specific to doxepin, however, should take into account the possibility of these reactions because of the similarity of its pharmacological properties with other tricyclic agents
Adverse Reactions distributed frequency manifestations: very common (> 1/10). often (> 1/100, < 1/10), rare (> 1/1000, < 1/100), rare (> 1/10 000, < 1/1000), very rare (> 1/10 000), not known (frequency can not be determined according to available information)
From the nervous system and mental disorders .. very often ; drowsiness; rare ; headache, dizziness, insomnia, nightmares, confusion, disorientation, anxiety, numbness or paresthesia, tremor (usually of moderate severity). In applying the drug in high doses (especially in elderly patients) may have extrapyramidal symptoms, including tardive dyskinesia; rare ; hallucinations, ataxia (generally used when several drugs acting on the central nervous system), convulsions (in patients who are prone to the emergence of seizures, the cause of which may be damage to the brain or the use of alcohol and substance abuse); known ; suicidal thoughts and behavior. Reported cases of suicidal thoughts and behavior during treatment with doxepin or immediately after its cancellation.
The mental symptoms, including delusions and paranoid delusions, can be amplified in the treatment of tricyclic antidepressants. Occasionally reported ringing in the ears.
From a sight organ . very rare ; visual disturbances (blurred)
From the circulatory system: rare ;. orthostatic hypotension, flushing.
From the of the heart. very rare ; tachycardia, ECG disturbances (extension set QRS lengthening of the interval P –. R ).
From the of the immune system. rare ; allergic reactions including rash, swelling of the face, increased photosensitivity, pruritus, urticaria. During treatment with tricyclic antidepressants may increase asthma.
Skin and subcutaneous tissue . rare ; increased sweating, allergic skin reactions as defined above; very rare ; alopecia.
From the blood system and the lymphatic system . rare ; eosinophilia and bone marrow disorders with symptoms such as agranulocytosis, leukopenia, thrombocytopenia, purpura and hemolytic anemia.
From the digestive system . very often ; dry mucous membranes of the mouth and nose, constipation; rare ; nausea, vomiting, dyspepsia, taste disturbance, diarrhea, anorexia, stomatitis.
From endocrine system . rare ; inappropriate secretion of antidiuretic hormone, gynecomastia, breast enlargement, galactorrhea in females; isolated cases ; changes in libido, testicular swelling, increase or decrease the level of glucose in the blood.
From the kidneys and urinary system . rare ; urinary retention (in men with prostatic hypertrophy complaints may worsen).
From the hepatobiliary system . rare ; jaundice.
General disorders . very often ; fatigue, weakness, weight gain, chills, hyperpyrexia (in patients taking both chlorpromazine).
Cancel doxepin . With the sudden cancellation of tricyclic antidepressants may experience withdrawal symptoms, including insomnia, irritability and excessive sweating. Withdrawal symptoms in newborns whose mothers took tricyclic antidepressants in the III trimester include inhibition of the respiratory function, hyperreflexia and convulsions.
Patients with concomitant diseases or those taking other medications, you should apply a single dosing regimen. This also applies to patients who use drugs with anticholinergic action.
For the elderly should also use this mode of dosing and with care to correct it. These patients are prone to develop adverse reactions such as anxiety, confusion, and orthostatic hypotension. Therefore, the starting dose should be administered with caution and under close supervision of the patient’s condition and response to the drug. For the corresponding clinical effect can be quite half-dose doxepin.
Patients should be warned that during treatment can occur drowsiness and alcohol intake can enhance the effects of the drug.
In case of deterioration of psychotic symptoms or manic episodes in the treatment of doxepin may . require a reduction in dose or adding to the treatment regimen of drugs group tranquilizers (neuroleptics)
Although the use of doxepin less effect on the vascular system than other tricyclic antidepressants, should be used with caution in patients with severe cardio – vascular diseases (heart block, cardiac arrhythmia, and recent myocardial infarction).
It takes careful when using doxepin in patients with renal impairment, liver and those with a history of seizures.
Suicide / suicidal thoughts or clinical worsening . Patients with major depression there is a risk of suicidal thoughts and actions, which may persist until remission. In the case where no improvement occurs within the first few weeks of treatment, or even more, patients should be closely monitored until such time when it’s status improved. Out of the total clinical practice it is known that the risk of suicidal thoughts or actions may increase in the early stages of treatment.
In other psychiatric conditions for which treatment is prescribed doxepin, as there is an increased risk of suicide cases. Therefore, special precautions must be observed for these patients.
Careful monitoring during the treatment of patients with suicidal thoughts or attempts of suicide in history.
Careful monitoring of patients, especially high-risk groups, should be combined with appropriate medicines, especially in the early stages, followed if necessary changing dosing. Required to inform patients (and those who lead their observation) the need to monitor if any clinical worsening, suicidal behavior or thoughts unusual changes in behavior and to seek immediate medical attention in the event of these symptoms
A meta-analysis of placebo -. Controlled research at the use of antidepressants in adult patients with psychiatric disorders showed increased risk of suicidal behavior in patients under the age of 25 years compared with placebo.
in patients with prostatic hypertrophy moderate severity may increase urinary retention.
doxepin contains lactose monohydrate, therefore patients with rare hereditary forms of intolerance to galactose malabsorption of glucose and galactose, Lapp lactase deficiency is not recommended to assign.
patients with hypersensitivity or intolerance to gluten should not use this drug as part of its subsidiary substances include starch
Use during pregnancy or breast-feeding The study of the reproductive function in animals have revealed adverse effects on the fetus..; adequate and clear-controlled studies in pregnant women have been conducted. Thus, during the period of pregnancy, the drug is used only in cases where the expected benefit to the mother outweighs the potential risk to the fetus.
Doxepin passes into breast milk, so during treatment should stop breastfeeding.
Children . the safety and efficacy of doxepin in children have not been established.
the ability to influence the rate of reaction when driving or operating other machines. during treatment, doxepin is prohibited to drive vehicles or work with complex mechanisms that require concentration, because the drug can cause drowsiness and other negative reactions on the part of the central nervous system.
, while the use of ethanol, antidepressants, barbiturates, benzodiazepines and general anesthetics may significantly increased inhibitory action on CNS, respiratory depression and hypotensive effect. Doxepin increases the anticholinergic effects of amantadine. Phenothiazines, antiparkinsonian drugs, atropine, biperiden, antihistamines increase the risk of side effects from the central nervous system, eyes, intestines, bladder. In an application with antihistamines, clonidine enhanced inhibitory effect on the CNS, with atropine ; increased risk of paralytic ileus, with drugs that cause extrapyramidal reactions, ; increased body weight and frequency of extrapyramidal effects. With simultaneous use of doxepin with indirect anticoagulants (coumarin derivatives or indadiona) may increase the anticoagulant activity of the latter. Doxepin may exacerbate depression caused by corticosteroids. The combined application with anticonvulsants may increase depressant effects on the central nervous system, decrease seizure threshold (when used in high doses) and a decrease in the efficiency of the latter. Preparations for the treatment of hyperthyroidism increases the risk of agranulocytosis. Doxepin reduces the effectiveness of phenytoin and alpha – blockers. Inhibitors of microsomal oxidation (cimetidine), extend T ½. increase the risk of toxic effects doxepin (may require dose reduction doxepin 20 – 30%), inducers of microsomal liver enzymes (barbiturates, carbamazepine, phenytoin, nicotine and oral contraceptives) reduce the concentration in plasma and the effectiveness of doxepin. Fluoxetine and fluvoxamine doxepin increase the concentration in plasma (doxepin may require dose reduction by 50%). In an application with holinoblokatorami, phenothiazines and benzodiazepines ; mutual reinforcement of the central sedative and anticholinergic effects and increased risk of seizures (decrease seizure threshold); phenothiazines, moreover, can increase the risk of neuroleptic malignant syndrome. With simultaneous use of doxepin with clonidine, guanethidine, betanidinom, reserpine and methyldopa ; decrease the hypotensive effect of the latter; cocaine ; the risk of cardiac arrhythmias. Estrogensoderjath oral contraceptives and estrogens may increase the bioavailability of doxepin; antiarrhythmics (quinidine) increase the risk of arrhythmias (possibly slowing metabolism of doxepin). Concomitant use with disulfiram and inhibitors atsetaldegidrogenazy provoke delirium. Incompatible with MAO inhibitors (possible increase in the frequency of periods hyperpyrexia, severe convulsions, hypertensive crisis and death of the patient). And pimozide probucol may increase the cardiac arrhythmia that is shown lengthening the interval Q – T on the ECG. There is a growing effect on the cardio – vascular system of epinephrine, norepinephrine, isoprenaline, ephedrine and phenylephrine (including when these funds are part of local anesthetics), and increases the risk of cardiac arrhythmias, tachycardia, severe hypertension. The simultaneous use of blockers α – adrenoceptor for intranasal administration or for use in ophthalmology (with significant systemic absorption), may enhance the vasoconstrictor action of the latter. The combined application with thyroid hormones ; mutual enhancement of therapeutic effects and toxic effects (including cardiac arrhythmia and a stimulating effect on the CNS). M – holinoblokatory and antipsychotics increase the risk of hyperpyrexia (especially in hot weather).
symptoms: drowsiness, anxiety, dry mouth, stupor, visual disturbances, arrhythmia. If you have any of these symptoms the drug should be discontinued and the patient survey.
In severe overdose may be a decrease / increase in blood pressure, dilated pupils, tachycardia, urinary retention (atonic bladder), ileus, hyperthermia / hypothermia, respiratory depression, sweating, seizures , coma
Treatment: discontinuation of the drug, gastric lavage, artificial ventilation, control of cardio – vascular system, the use of hypnotics.. If necessary ; administration of physostigmine salicylate 1 – 3 mg. Symptomatic therapy. Hemodialysis and forced diuresis are not effective.
at a temperature not higher than 25 ° C in a dark place.
Date Modified: 20/01/2016