Posts Tagged ‘Eicosanoids’

What is Unoprostone

Saturday, December 6th, 2008

Unoprostone (INN) is a prostaglandin analogue. Its isopropyl ester, unoprostone isopropyl, is marketed under the trade name Rescula (eyedrops, 0.15%) for the management of open-angle glaucoma and ocular hypertension.

Important safety information of Treprostinil

Saturday, December 6th, 2008

Since treprostinil is a vasodilator, its antihypertensive effect may be compounded by other medications that affect the blood pressure, including calcium channel blockers, diuretics, and other vasodilating agents.
Because of treprostinil’s inhibiting effect on platelet aggregation, there is an increased risk of bleeding, especially among patients who are also taking anticoagulants.
It is not known whether treprostinil is excreted in breast milk. Caution is advised when administering this medication to nursing women.
Caution is advised when administering treprostinil to patients who have impaired kidney or liver function.

Common side effects:
85% of patients report pain or other reaction at the infusion site. Other side effects may include headache, diarrhea, nausea, rash, jaw pain, vasodilatation, dizziness, edema (swelling), pruritus (itching), and hypotension.

Warnings:

Dosage and administration of Treprostinil

Saturday, December 6th, 2008

Treprostinil is administered via a small infusion pump that the patient must wear at all times. Treprostinil is preferentially given subcutaneously using an infusion set, but may be given intravenously via a central venous catheter if the patient is unable to tolerate the potential pain and discomfort of subcutaneous administration.

Treprostinil, under the trademark Remodulin, is supplied in 20 mL vials, ranging in concentrations of 1 mg/mL, 2.5 mg/mL, 5 mg/mL, and 10 mg/mL. Treprostinil can be administered subcutaneously as supplied. It must be diluted for intravenous infusion with either sterile water or a 0.9% sodium chloride solution prior to administration.

The infusion rate is normally initiated at 1.25 ng/kg/min for new patients, but may be reduced to 0.625 ng/kg/min if the normal rate provokes unwanted side effects in the patient. The infusion rate of trepostinil should be increased no more than 1.25 ng/kg/min per week for the first month, then no more than 2.5 ng/kg/min per week for the remaining duration of infusion. The infusion rate should ideally be high enough to improve symptoms of pulmonary hypertension, while minimizing unpleasant side effects.

Oral and inhaled forms of treprostinil are currently undergoing clinical trials.

Clinical pharmacology of Treprostinil

Saturday, December 6th, 2008

As an analogue of prostacyclin PGI2, treprostinil effects vasodilation, which in turn lowers the blood pressure. Treprostinil also inhibits platelet aggregation, though the role this phenomenon may play in relation to pulmonary hypertension has yet to be determined.

What is Treprostinil

Saturday, December 6th, 2008

Treprostinil is a synthetic analogue of prostacyclin, used to treat pulmonary hypertension. Treprostinil is marketed as Remodulin.

What is Travoprost

Saturday, December 6th, 2008

Travoprost ophthalmic solution is a topical medication used for controlling the progression of glaucoma or ocular hypertension, by reducing intraocular pressure. It is a prostaglandin analogue that works by increasing the outflow of aqueous fluid from the eyes.[1] It is also known by the brand name of Travatan, manufactured by Alcon Inc. Travoprost is a synthetic prostaglandin F 2? analogue. Its chemical name is isopropyl (Z)-7- [(1 R ,2 R ,3 R ,5 S )-3,5-dihydroxy-2-[(1 E ,3 R )-3-hydroxy-4-[(?,?,?-trifluoro- m -tolyl)oxy]-1- butenyl]cyclopentyl]-5-heptenoate.[2]Travoprost ophthalmic solution is a topical medication used for controlling the progression of glaucoma or ocular hypertension, by reducing intraocular pressure. It is a prostaglandin analogue that works by increasing the outflow of aqueous fluid from the eyes.[1] It is also known by the brand name of Travatan, manufactured by Alcon Inc. Travoprost is a synthetic prostaglandin F 2? analogue. Its chemical name is isopropyl (Z)-7- [(1 R ,2 R ,3 R ,5 S )-3,5-dihydroxy-2-[(1 E ,3 R )-3-hydroxy-4-[(?,?,?-trifluoro- m -tolyl)oxy]-1- butenyl]cyclopentyl]-5-heptenoate.[2]

What is Tafluprost

Saturday, December 6th, 2008

Tafluprost (trade name Taflotan, marketed by Santen Pharmaceutical Co.) is a prostaglandin analogue used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension. It reduces intraocular pressure by increasing the outflow of aqueous fluid from the eyes.[1][2]

Taflotan contains 15 µg/ml Tafluprost. Taflotan sine is a preservative-free, single-dose formulation containing 0.3 ml per dose.[3]

Uses of Prostaglandin analogue

Saturday, December 6th, 2008

Prostaglandin analogues such as misoprostol are used in treatment of duodenal and gastric ulcers. They exert antisecretory and cytoprotective properties and are especially indicated for the elderly on continuous doses of NSAIDs.
Prostaglandin analogues can also be used in the management of open-angle glaucoma. They reduce intra-ocular pressure by enhancing uveoscleral outflow and may also have some effect on the trabecular meshwork as well. Latanoprost, travoprost, unoprostone and bimatoprost are examples of prostaglandin analogues used in the management of open-angle glaucoma. In some countries such as Australia, they are now considered first line agents in open-angle glaucoma (rather than beta blockers)[1]

What is Prostaglandin analogue

Saturday, December 6th, 2008

Synthetic prostaglandin analogues are molecules which are manufactured to bind to a prostaglandin receptor.

Wider use of prostaglandin analogues is limited by unwanted side effects and their abortive potential.

What is Prostaglandin H2

Saturday, December 6th, 2008

Prostaglandin H2 is a type of Prostaglandin which is derived from arachidonic acid and is a precursor for many other biologically significant molecules: