''S''-Ethylisothiouronium diethylphosphate (brand name Difetur) is an ''S''-alkylisothiouronium derivative used as an

antihypotensive An antihypotensive agent, also known as a vasopressor agent or simply vasopressor, or pressor, is any substance, whether endogeny (biology), endogenous or a medication, that tends to raise low blood pressure. Some antihypotensive drugs act as vas ...

drug. The ''S''-alkylisothiouronium compounds are used in processes of treating acute hypotension, which may result, for example, from shock or hemorrhage, and in processes for treating hyperoxic conditions, for example, oxygen poisoning.

Indications

It is used for increasing arterial blood pressure in cases of acute arterial hypotension due to surgical interference, trauma, poisoning, shock condition, hemorrhages; in conjunction with epidural anesthesia; in overdose of ganglion blockers, alpha-adrenergic blockers, neuroleptics, anesthetics; and in other conditions when adrenomimetics are contra-indicated or ineffective. Difetur was also found to possess oxygen protective activity and, thus, can be used as a medicament for protecting against oxygen poisoning conditions caused by hyperoxia. ''S''-Ethylisothiouronium diethylphosphate is also used for the treatment of headaches, in particular, migraines, as well as for the prevention or treatment of nausea and vomiting, effective in preventing or alleviating emesis associated with migraines or other medical conditions such as chemotherapy or radiotherapy, as well as other symptoms of migraines including phonophobia and photophobia.

Mechanism of action

''S''-Ethylisothiouronium diethylphosphate is a specific inhibitor of

inducible NO synthase Nitric oxide synthases () (NOSs) are a family of enzymes catalyzing the production of nitric oxide (NO) from L-arginine. NO is an important cellular signaling molecule. It helps modulate vascular tone, insulin secretion, airway tone, and peri ...

on hepatic NO production level. ''S''-Ethylisothiouronium diethylphosphate affects systemic hemodynamic indices in the following way: the peripheral vascular resistance increases, the stroke volume and central blood volume increase, and the work of the left ventricle improves. Other effects are:

analgesic An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It ...

uterotonic A uterotonic, also known as ecbolic, are pharmacological agents used to induce contraction or greater tonicity of the uterus. Uterotonics are used both to induce labor and to reduce postpartum hemorrhage. Labor induction in the third trimester of ...

, decongestive and

anti-inflammatory Anti-inflammatory is the property of a substance or treatment that reduces inflammation or swelling. Anti-inflammatory drugs, also called anti-inflammatories, make up about half of analgesics. These drugs remedy pain by reducing inflammation as o ...

. In difetur’s antihypotensive effect unlike

sympathomimetics Sympathomimetic drugs (also known as adrenergic drugs and adrenergic amines) are stimulant compounds which mimic the effects of endogenous agonists of the sympathetic nervous system. Examples of sympathomimetic effects include increases in heart ...

there is no stimulation of the

sympathetic system The sympathetic nervous system (SNS) is one of the three divisions of the autonomic nervous system, the others being the parasympathetic nervous system and the enteric nervous system. The enteric nervous system is sometimes considered part of the ...

, thus does not cause

tachycardia Tachycardia, also called tachyarrhythmia, is a heart rate that exceeds the normal resting rate. In general, a resting heart rate over 100 beats per minute is accepted as tachycardia in adults. Heart rates above the resting rate may be normal (su ...

, nor alter the acid-base balance and electrolyte and does not cause hypotension secondary. These drugs have also sedative action, reduce body temperature and oxygen consumption.

Forms

Injectable solution 10%-1 ml in ampules N 10.

References

{{DEFAULTSORT:Ethylisothiouronium diethylphosphate, S- Organophosphates Antihypotensive agents