Dosulepin

Dosulepin

File:Dosulepin (cis,trans-mixture) Structural Formulae.png
Systematic (IUPAC) name
(E,Z)-3-(dibenzo[b,e]thiepin-11(6H)-ylidene)-N,N-dimethylpropan-1-amine
Clinical data
Pregnancy category	C
Routes of administration	Oral
Legal status
Legal status	℞ (Prescription only)
Pharmacokinetic data
Bioavailability	30%
Metabolism	Hepatic
Biological half-life	20 hours
Excretion	Renal
Identifiers
CAS Number	113-53-1
ATC code	N06AA16 (WHO)
PubChem	CID 13473
Chemical data
Formula	C19H21NS
Molar mass	295.45 g/mol[[]]

Dosulepin (INN), formerly known as dothiepin (BAN), is a tricyclic antidepressant (TCA). It is sold under the brand names Prothiaden, Dothep, Thaden and Dopress. Dosulepin blocks the reuptake of serotonin and norepinephrine in the brain, thereby increasing their levels. It is believed that this action is responsible for its mood-elevating effects.

Indications

Dosulepin is relatively mild and is used for low-level anxiety, depression and similar disorders, as well as the treatment of chronic and ongoing pain disorders, particularly where insomnia and/or loss of appetite are present. It can take between two and four weeks of regular usage to become effective; it is often started at a low level and the dosage increased if this is ineffective. The drug causes drowsiness as a side-effect, and this may be used as part of the treatment, since anxiety-depressive patients may have difficulty sleeping; it can also be combined with other drugs such as temazepam.

Dosage

Adults: Initially 75 mg/day in divided doses or as a single dose at night, increasing to 150 mg/day. In certain circumstances, e.g. in hospital use or unresponsive patients, dosages up to 300 mg daily have been used.

Suggested regimens: 25 or 50 mg three times daily or, alternatively, 75 or 150 mg as a single dose at night. Should the regimen of 150 mg as a single night-time dose be adopted, it is better to give a smaller dose for the first few days.

Elderly: 50 to 75 mg daily initially. As with any antidepressant, the initial dose should be increased with caution under close supervision. Half the normal adult dose may be sufficient to produce a satisfactory clinical response.

Children: Not recommended.

Side effects

The most common side effects are drowsiness and dry mouth as well as dry eyes. Other less common side effects may include:

• dizziness
• Blurred vision
• Tachycardia
• Urinary retention
• Tremors, especially of the hands
• Blood disorders
• Hypotension
• Sexual dysfunction
• Sweating
• Increased sensitivity to sunlight and increased vulnerability to sunburn

These side effects cease when treatment ceases. Alcohol should be avoided whilst taking dosulepin as it may increase some side-effects.

Whilst dosulepin is not addictive, it should not be stopped suddenly as there is a risk of initial withdrawal symptoms which may be mistaken for some of the original indications for the drug:

• Nausea
• Vomiting
• Loss of appetite
• Headache
• Giddiness
• Chills
• Insomnia
• Anxiety

Contraindications

Contra indications include:

• Certain conditions of the heart, mainly those affecting the electrical impulses to the heart muscle, particularly arrhythmia or recent heart attack
• Mania.
• Liver disease or thyroid disease
• Epilepsy, phaeochromocytoma, glaucoma or diabetes
• Hypotension, vulnerability to dizziness or fainting
• History of urinary retention or porphyria

Drug interactions

The drug can interact dangerously with vasoconstrictors and should not be taken in combination with phenylephrine or adrenaline in particular.

The sedative effects of other CNS depressants (benzodiazepines such as diazepam and lorazepam, sedative antihistamines, opiates, etc.) may be increased.

This drug should not be started within 2 weeks of stopping a monoamine oxidase inhibitor (MAOI) antidepressant, and should not be co-administered with any selective serotonin reuptake inhibitor (SSRI) antidepressant such as fluoxetine), or any medication which affects the electrical impulses to the heart (e.g. astemizole, halofantrine or terfenadine).

The drug is not recommended for use by children nor to be taken in combination with some other drugs, including herbal remedies.

Overdose

Main article: Tricyclic antidepressant overdose

The symptoms and the treatment of an overdose are largely the same as for the other tricyclic antidepressants.

Chemistry

Dosulepin is made as follows: 500px

Zirkle, C. L.; 1971, U.S. Patent 3,609,167.

See also

• Tricyclic antidepressant

References

de:Dosulepin ru:Амитриптилин