Rectogesic - General Information
A volatile vasodilator which relieves angina pectoris by stimulating guanylate cyclase and lowering cytosolic calcium. [PubChem]
Pharmacology of Rectogesic
Rectogesic, an organic nitrate, is available in many forms as a vasodilator. Rectogesic is used in the treatement of angina pectoris and perioperative hypertension, to produce controlled hypotension during surgical procedures, to treat hypertensive emergencies, and to treat congestive heart failure associated with myocardial infarction.
Rectogesic for patients
Daily headaches sometimes accompany treatment with nitroglycerin. In patients who get these headaches, the headaches may be a marker of the activity of the drug. Patients should resist the temptation to avoid headaches by altering the schedule of their treatment with nitroglycerin, since loss of headache may be associated with simultaneous loss of antianginal efficacy.
Treatment with nitroglycerin may be associated with lightheadedness on standing, especially just after rising from a recumbent or seated position. This effect may be more frequent in patients who have also consumed alcohol.
After normal use, there is enough residual nitroglycerin in discarded patches that they are a potential hazard to children and pets.
A patient leaflet is supplied with the systems.
The vasodilating effects of nitroglycerin may be additive with those of other vasodilators. Alcohol, in particular, has been found to exhibit additive effects of this variety.
Marked symptomatic orthostatic hypotension has been reported when calcium channel blockers and organic nitrates were used in combination. Dose adjustments of either class of agents may be necessary.
Use of Transderm-Nitro (nitroglycerin) transdermal system is contraindicated in patients
using Viagra (sildenafil) because sildenafil may amplify the vasodilatory effects of
Transderm-Nitro resulting in severe hypotension.
Allergic reactions to organic nitrates are extremely rare, but they do occur. Nitroglycerin
is contraindicated in patients who are allergic to it. Allergy to the adhesives used in
nitroglycerin patches has also been reported, and it similarly constitutes a contraindication
to the use of this product.
Additional information about Rectogesic
Rectogesic Indication: For the prevention of angina
Mechanism Of Action: Similar to other nitrites and organic nitrates, nitroglycerin is converted to nitric oxide (NO), an active intermediate compound which activates the enzyme guanylate cyclase. This stimulates the synthesis of cyclic guanosine 3',5'-monophosphate (cGMP) which then activates a series of protein kinase-dependent phosphorylations in the smooth muscle cells, eventually resulting in the dephosphorylation of the myosin light chain of the smooth muscle fiber. The subsequent release of calcium ions results in the relaxation of the smooth muscle cells and vasodilation.
Drug Interactions: Alteplase IV nitroglycerin decreases the effect of alteplase
Dihydroergotamine Possible antagonism of action
Dihydroergotoxine Possible antagonism of action
Ergonovine Possible antagonism of action
Ergotamine Possible antagonism of action
Methylergonovine Possible antagonism of action
Methysergide Possible antagonism of action
Sildenafil Possible significant hypotension with this combination
Tadalafil Possible significant hypotension with this combination
Vardenafil Possible significant hypotension with this combination
Food Interactions: Avoid alcohol.
Take on empty stomach: 1 hour before or 2 hours after meals.
Dissolve under the tongue.
Generic Name: Nitroglycerin
Synonyms: TNG; NTG; NG; Nitroglycerine; Trinitroglycerin; Glyceryl trinitrate
Drug Category: Tocolytic Agents; Vasodilator Agents; Nitrates and Nitrites
Drug Type: Small Molecule; Approved; Investigational
Absorption: Not Available
Toxicity (Overdose): Increased intracranial pressure, with any or all of persistent throbbing headache, confusion, and moderate fever; Vertigo; Palpitations; Visual disturbances; Nausea and vomiting (possibly with colic and even bloody diarrhea); Syncope (especially in the upright posture); Air hunger and dyspnea, later followed by reduced ventilatory effort; Diaphoresis, with the skin either flushed or cold and clammy; Heart block and bradycardia; Paralysis; Coma; Seizures; Death.
Protein Binding: Not Available
Biotransformation: Hepatic, cytochrome P450 (P450) is a key enzyme of organic nitrate biotransformation
Half Life: 3 minutes
Dosage Forms of Rectogesic: Solution Intravenous
Aerosol, metered Sublingual
Spray, metered Sublingual
Solution / drops Oral
Chemical IUPAC Name: 1,3-dinitrooxypropan-2-yl nitrate
Chemical Formula: C3H5N3O9
Nitroglycerin on Wikipedia: https://en.wikipedia.org/wiki/Nitroglycerin
Organisms Affected: Humans and other mammals