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Prostaglandins and analogues

Agonists of prostaglandin receptors include prostaglandins themselves and analogues, they are direct acting prostaglandinomimetics. Only products which induce beneficial effects are used in therapeutics. The difficulty was to obtain sufficient quantity of active compounds in a sufficiently stable form and with a sufficient long-lasting action.

One can classify prostaglandins according to their therapeutic uses, cardiovascular, digestive, gynecological, obstetrical or ophthamic.

Cardiovascular uses

PGI2 or prostacyclin, called now epoprostenol, has several interesting properties: pulmonary and systemic arterial vasodilator, platelet anti-aggregating, gastric protective effects.

In sustained continuous intravenous infusion it induces appreciable results in the treatment of primitive pulmonary arterial hypertension. It is not active by oral route.

epoprostenol

FLOLAN * I

Iloprost, a stable analog of PGI2, is used for the treatment of severe peripheral vascular disease. In aerosol it gave interesting results in the treatment of primitive pulmonary hypertension. Its most frequent adverse effects are flushes and headache.

Alprostadil (PGE1) is indicated for keeping the ductus arteriosus open until surgery in neonates carrying certain cardiac malformations. Because of its vasodilator effect, alprostadil is also used by intracavernous route for the treatment of erectile dysfunction

Alprostadil (PGE1 type)

CAVERJECT * Intracavernosal administration
MUSE* Urethral administration

Digestive uses

Misoprostol, an analog of PGE1, has antisecretory and cytoprotector gastric effects. It decreases acid secretion and increases pepsin, mucin and bicarbonate secretion and improves microcirculation. It is indicated in the treatment of gastroduodenal ulcer and for the prevention of NSAID-induced ulcers. Its principal secondary effect is diarrhea. It is contra-indicated for pregnant women.

Misoprostol ( typeE1)

CYTOTEC * Tablets

Gynecological and obstetrical uses

The derivatives used in gynecology and obstetrics have an activity which resembles that of the prostaglandins E1 and E2.  They induce cervical dilatation and uterine contractions, particularly in late pregnancy.

  • E1 type
    G emeprost is used for dilatating the cervix for uterine exploration or abortion.
  • E2 type
    D inoprostone is used in low doses for inducing labor in late pregnancy, with higher doses to elicit an abortion or a therapeutic interruption of pregnancy. In the cervical gel formulation, it is used obtain cervix dilatation.

    Dinoprostone (E2 type)

    CERVIDIL*

Sulprostone is used in intravenous perfusion or intramuscular injection to elicit abortion, in combination with mifepristone which is an antiprogestin. It induced coronary spasms and of myocardial infarction. It is contra-indicated in women who smoke or over 35.

The gynecological and obstetrical therapeutic uses correspond to uses of short duration. Their adverse effects are nausea, vomiting, headache, hot flashes.

Ophthalmologic uses

Latanoprost, a prodrug analog of F2 alpha prostaglandin, administered in ophthalmic solution, lowers intraocular pressure by increasing aqueous humor outflow by the uveoscleral route. Secreted by the ciliary body, the aqueous humor reaches the anterior chamber from which it is eliminated by the trabecular route (channel of Schlemm) and the uveoscleral route.

At the dose of a drop of ophthalmic solution per day, latanoprost lowers ocular pressure by approximately 30% in most patients with open-angle glaucoma.

Latanoprost, used during several months, causes in certain patients – especially in those with brown eyes, a change of eye color, a browning of the iris, by increase in the amount of melanin in cells. Before prescribing latanoprost, it is necessary to inform the patient of the possibility of this color change which, if it is unilateral, causes heterochromy. Darkening of eyelids and eyelashes has also been described. Like the F2a prostaglandin, latanoprost, after diffusion in the body, could have a bronchoconstrictor effect perceptible in asthmatic patients.

Latanoprost
Latanoprost + Timolol
XALATAN * Ophthalmic solution
XALACOM * Ophthalmic solution

Bimatoprost

LUMIGAN * Ophthalmic solution

Travoprost

TRAVATAN * Ophthalmic solution

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Quizz : Q 13
PGI2, also called prostacyclin or epoprostenol
induces vasodilation
prevents platelet aggregation 
has a broncho-constrictor effect
is used by oral route
can be used for the treatment of pulmonary arterial hypertension

... more quizz
157 In order to reduce the gastrointestinal a...
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