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(October 2007)DoxepinSystematic (IUPAC) name3-(dibenzooxepin-11(6H)-ylidene)-N,N-dimethylpropan-1-amineIdentifiersCAS number1668-19-5ATC codeN06AA12PubChem3158DrugBankAPRD00398ChemSpider3046Chemical dataFormulaC19H21NO Mol. mass279.376 g/molPharmacokinetic dataBioavailabilityAbsolute = 25%When main metabolite desmethyldoxepin is included: 31%MetabolismHepaticHalf lifeDoxepin 17h, main metabolite Desmethyldoxepin 51hExcretionRenalTherapeutic considerationsPregnancy cat.Not recommended.Animal studies have shown embryotoxic properties.Legal status℞ Prescription onlyRoutesOral, intramuscular injection, intravenous infusionDoxepin (IPA: /ˡdɑːksəˌpɪn/, DAAK-sə-PIN) is a psychotropic agent with tricyclic antidepressant and anxiolytic properties, known under many brand-names such as Aponal, the original preparation by Boehringer-Mannheim, now part of the Roche group; Adapine, Deptran, Sinquan and Sinequan (Pfizer). As doxepin hydrochloride it is the active ingredient in cream based preparations (Zonalon and Xepin) for the treatment of dermatological itch. Doxepin is currently investigated for the treatment of insomnia, and the proposed tradename of doxepin for this indication is Silenor.// PharmacologyDoxepin inhibits the reuptake of serotonin and noradrenaline from the synaptic cleft (dual action). The reuptake-inhibition of dopamine is very weak.It has antagonistic effects (blockade) on a variety of postsynaptic receptors:Extremely strong : histaminic H1, H2Strong : serotonergic 5-HT2, adrenergic alpha1, muscarinicModerate : serotonergic 5-HT1Weak : dopaminic D2, adrenergic alpha2These effects account for the actions as well for most side-effects (sedation, hypotension, anticholinergic side-effects, weight gain). Doxepin shows strong antagonism against the effects of reserpine (amine depletion) in the animal model. Like other 'classical' antidepressants it has a sodium channel blocking activity, possibly accounting for its analgesic action. Additionally, Doxepin exerts a strong local-anesthetic action.Peak plasma levels are seen 2 to 3 hours after oral dosing. ToxicologyMouse : i.v. 15 - 20 mg/kg body weight, oral 148 - 178 mg/kg body weightRat : i.v. 13 - 19 mg/kg body weight, oral 346 - 460 mg/kg body weightHuman : Not exactly known, clinical experience indicates a rather high acute toxicity, as is the case with other tri-/tetracyclics. Fatal dose in sensitive adults may be as low as 500 to 1,000 mg oral (7 to 14 mg/kg). In children below 12 yrs. of age any oral intake is to be considered as serious.Dog and Rat : Fat deposits in liver cells and decrease of triglyceride levels in plasmaHuman : Data not available IndicationsApproved uses may vary by country. In the United States, the only Food and Drug Administration (FDA) approved use of doxepin is in the treatment of depression. All other uses are considered off-label.Major depressionAnxiety disorder, longterm-treatment is possible.Insomnia, also suitable for long-term treatment.Alleviation of the symptoms of alcohol and drug withdrawal (N.B.: Doxepin does not suppress seizure activity in alcoholics (delirium tremens). Cotreatment with benzodiazepines or barbiturates is needed to treat seizures effectively.Gastrointestinal ulceration and other GI-problems (e.g. irritable bowel syndrome), whether part of depression or not. The action is due to strong H2-receptor antagonism. The efficiacy is comparable to H2-Receptor-Inhibitors.Chronic pain, particular tension headaches, whether associated with depression or notTopical (external) treatment of itching skin disease with Zonalon and Xepinlow dose doxepin (3 to 6 mg) is currently on phase 3 as "new" treatment for insomnia. Contraindicationsknown hypersensitivity to doxepin or other dibenzoxepines or other ingredients of the drugacute intoxication with alcohol, sedatives, analgesics and other psychoactive drugsacute delirium tremensuntreated closed angle glaucomahypertrophy of the prostate with urine retentionparalytic ileushypertrophy of the prostate without urine retentionreduced function of the bone marroworganic brain disordersincreased risk of seizures, preexisting epilepsypreexisting cardial damage, particular some arrhythmias (e.g. sinoatrial blockage)other forms of preexisting cardiac damage (other arrhythmias, insufficience)MAO-Inhibitors of the irreversible type (tranylcypromine among others) : These drugs should normally be stopped at least 2 weeks before therapy with doxepin is started.Children under 12 years of age should not be treated, because no sufficient clinical experience exists for this group of age. Tricyclic antidepressant drugs, particularly when given in high doses, can induce sinus tachycardia, changes in conduction time and arrhythmias. A few instances of unexpected death have been reported in patients with cardiovascular disorders. Myocardial infarction and stroke have also been reported with drugs of this class. Therefore, doxepin should be administered with extreme caution to patients with a history of cardiovascular disease, those with circulatory lability and elderly patients. In such cases, treatment should be initiated with low doses with progressive increases only if required and tolerated, and the patients should be under close surveillance at all dosage levels. Since tricyclic agents are known to reduce the seizure threshold, doxepin should be used with caution in patients with a history of convulsive disorders. Concurrent administration of ECT and doxepin may be hazardous and, therefore, such treatment should be limited to patients for whom it is essential. Close supervision is required when doxepin is given to hyperthyroid patients or those receiving thyroid medication because of the possibility of cardiovascular toxicity. At doses above 150 mg/day, it may block the antihypertensive effect of guanethidine and related compounds. PrecautionsBefore initiation of treatment a complete and differentiated blood count should be taken. If any value is pathologic, the blood count should be monitored closely under therapy with doxepin. If values are normal, blood counts should be taken during therapy in regular intervals (recommended: weekly during first month of therapy, monthly during the next 2 months, every 3 months afterwards).Liver-function studies should be performed periodically. Pregnancy and lactationIf Doxepin is used chronically during pregnancy, the newborn may show a withdrawal syndrome with agitation, impaired cardio-respiratory functions, disturbed urination and defecation. Caution should be exerted in treating pregnant women on a regular basis.Doxepin is found in significant amounts in the milk of lactating women. If therapy is necessary, breastfeeding should be interrupted during treatment. In order to maintain supply, the mother may pump and discard the milk during her treatment. Side-effectsCentral Nervous System : fatigue, dizziness, drowsiness, lightheadedness, confusion, nightmares, agitation, increased anxiety, insomnia, seizures (infrequently), delirium, rarely induction of hypomania and schizophrenia (stop medication immediately), extrapyramidal side-effects (rarely), abuse in patients with polytoxikomania (rarely)Anticholinergic : dry mouth, obstipation, even ileus (rarely), difficulties in urinating, sweating, precepitation of glaucomaAntiadrenergic : hypotension, postural collapse (if patient arises too fast from lying/sitting position to standing), arrhythmias (sinus-tachycardia, bradycardia, av-blockade)Allergic/toxic : skin rash, photosensitivity, liver damage of the cholostatic type (rarely), hepatitis (extremely rare), leuko- or thrombopenia (rarely), agranulocytosis (very rarely), hypoplastic anemia (rarely)Others : frequently increased appetite, massive weight gain, rarely nausea, frequently impaired sexual function in men (impotence, ejaculation-difficulties), rarely hypertension, rarely polyneuropathy, in both sexes breast-enlargement and galactorrhea (rarely) Suicidal patientsPatients with suicidal thoughts, or those with previous suicidal attempts, should be monitored closely under treatment with Doxepin. Perhaps, the decision is made to hospitalize high risk patients until remission or to prescribe an additional sedating drug like a benzodiazepine or chlorprothixene for 2-4 weeks of initial treatment with Doxepin (until significant remission). At least, the smallest amount of Doxepin should be prescribed at one time to minimize the risk of deliberate overdose. Drug abuse and dependenceDoxepin has an extremely low potential for abuse and psychological dependence (mostly noted with polytoxicomaniacs, possibly due to the strong anxiolytic action of Doxepin).Withdrawal symptoms frequently seen when treatment with doxepin is stopped abruptly (agitation, anxiety, insomnia, sometimes activation of mania or rebound depression) are not indicative of addiction and can be avoided by reducing the daily dose of Doxepin gradually by approximately 25% each week. If treatment has to be stopped at once due to medical reasons, the use of a benzodiazepine (e.g. Lorazepam, Clonazepam, or Alprazolam) for a maximum of 4 weeks as needed will usually suppress withdrawal symptoms. Other remarksDoxepin may worsen psychotic conditions like schizophrenia and should be given with caution. The antipsychotic treatment should be continued.With Zonalon and Xepin; in most countries an external form (cream) is available for the treatment of itching skin disease; the effect is probably due to the affinity of doxepin for H1 and H2 receptors and action on muscarininc receptors. InteractionsIrreversible MAO-Inhibitors: agitation, delirium, coma, hyperpyrexia (high fever), seizures and

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