DRUGS & SUPPLEMENTS
Androskat usesAndroskat consists of Papaverine Hydrochloride, Phentolamine Mesylate.
This product is to be used by or under the direction of a physician.
Each vial contains a sufficient amount to permit withdrawal and administration of the volume specified on the label.
Androskat (Papaverine Hydrochloride), USP, is the hydrochloride of an alkaloid obtained from opium or prepared synthetically. It belongs to the benzylisoquinoline group of alkaloids. It does not contain a phenanthrene group as do morphine and codeine.
Androskat (Papaverine Hydrochloride), USP, is 6,7-dimethoxy-1- veratrylisoquinoline hydrochloride and contains, on the dried basis, not less than 98.5% of C20H21NO4-HCI. The molecular weight is 375.85. The structural formula is as shown.
Androskat (Papaverine Hydrochloride) occurs as white crystals or white crystalline powder. One gram dissolves in about 30 mL of water and in 120 mL of alcohol. It is soluble in chloroform and practically insoluble in ether.
Androskat (Papaverine Hydrochloride) Injection, USP, is a clear, colorless to pale-yellow solution.
Androskat (Papaverine Hydrochloride), for parenteral administration, is a smooth-muscle relaxant that is available in vials containing 30 mg/mL. Each vial also contains edetate disodium 0.005%. The 10 mL vials also contain chlorobutanol 0.5% as a preservative. pH may be adjusted with sodium citrate and/or citric acid.
The most characteristic effect of papaverine is relaxation of the tonus of all smooth muscle, especially when it has been spasmodically contracted. Androskat (Papaverine Hydrochloride) apparently acts directly on the muscle itself. This relaxation is noted in the vascular system and bronchial musculature and in the gastrointestinal, biliary and urinary tracts.
The main actions of papaverine are exerted on cardiac and smooth muscle. Papaverine relaxes various smooth muscles, especially those of larger arteries; this relaxation may be prominent if spasm exists. The antispasmodic effect is a direct one and unrelated to muscle innervation, and the muscle still responds to drugs and other stimuli causing contraction. Papaverine has minimal actions on the central nervous system, although very large doses tend to produce some sedation and sleepiness in some patients. In certain circumstances, mild respiratory stimulation can be observed, but this is therapeutically inconsequential. Papaverine stimulates respiration by acting on carotid and aortic body chemoreceptors.
Papaverine relaxes the smooth musculature of the larger blood vessels, including the coronary, cerebral, peripheral, and pulmonary arteries. This action is particularly evident when such vessels are in spasm, induced reflexly or by drugs, and it provides the basis for the clinical use of papaverine in peripheral or pulmonary arterial embolism.
Experimentally in dogs, the alkaloid has been shown to cause fairly marked and long-lasting coronary vasodilatation and an increase in coronary blood flow. However, it also appears to have a direct inotropic effect and, when increased mechanical activity coincides with decreased systemic pressure, increases in coronary blood flow may not be sufficient to prevent brief periods of hypoxic myocardial depression.
Papaverine is effective by all routes of administration. A considerable fraction of the drug localizes in fat deposits and in the liver, with the remainder being distributed throughout the body. It is metabolized in the liver. About 90% of the drug is bound to plasma protein. Although estimates of its biologic half-life vary widely, reasonably constant plasma levels can be maintained with oral administration at 6 hour intervals. The drug is excreted in the urine in an inactive form.
INDICATIONS AND USAGE
Papaverine is recommended in various conditions accompanied by spasm of smooth muscle, such as vascular spasm associated with acute myocardial infarction (coronary occlusion), angina pectoris, peripheral and pulmonary embolism, peripheral vascular disease in which there is a vasospastic element, or certain cerebral angiospastic states; and visceral spasm, as in ureteral, biliary, or gastrointestinal colic.
Intravenous injection of papaverine is contraindicated in the presence of complete atrioventricular heart block. When conduction is depressed, the drug may produce transient ectopic rhythms of ventricular origin, either premature beats or paroxysmal tachycardia.
Androskat (Papaverine Hydrochloride) is not indicated for the treatment of impotence by intracorporeal injection. The intracorporeal injection of Androskat (Papaverine Hydrochloride) has been reported to have resulted in persistent priapism requiring medical and surgical intervention.
Androskat Injection, USP, should not be added to Lactated Ringer’s Injection, because precipitation would result.
Androskat (Papaverine Hydrochloride) should be used with caution in patients with glaucoma. The medication should be discontinued if hepatic hypersensitivity with gastrointestinal symptoms, jaundice, or eosinophilia becomes evident or if liver function test values become altered.
Pregnancy Category C - No teratogenic effects were observed in rats when Androskat (Papaverine Hydrochloride) was administered subcutaneously as a single agent. It is not known whether papaverine can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Androskat (Papaverine Hydrochloride) should be given to a pregnant woman only if clearly needed.
It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Androskat is administered to a nursing woman.
Safety and effectiveness in children have not been established.
The following side effects have been reported: general discomfort, nausea, abdominal discomfort, anorexia, constipation or diarrhea, skin rash, malaise, vertigo, headache, intensive flushing of the face, perspiration, increase in the depth of respiration, increase in heart rate, a slight rise in blood pressure, and excessive sedation.
Hepatitis, probably related to an immune mechanism, has been reported infrequently. Rarely, this has progressed to cirrhosis.
DRUG ABUSE AND DEPENDENCE
Drug dependence resulting from the abuse of many of the selective depressants, including Androskat (Papaverine Hydrochloride), has been reported.
Signs and Symptoms –
The symptoms of toxicity from Androskat often result from vasomotor instability and include nausea, vomiting, weakness, central nervous system depression, nystagmus, diplopia, diaphoresis, flushing, dizziness, and sinus tachycardia. In large overdoses, papaverine is a potent inhibitor of cellular respiration and a weak calcium antagonist. Following an oral overdose of 15 g, metabolic acidosis with hyperventilation, hyperglycemia, and hypokalemia have been reported. No information on toxic serum concentrations is available.
Following intravenous overdosing in animals, seizures, tachyarrhythmias, and ventricular fibrillation have been reported. The oral median lethal dose in rats is 360 mg/kg.
To obtain up-to-date information about the treatment of overdose, a good resource is your certified Regional Poison Control Center. Telephone numbers of certified poison control centers are listed in the Physician’s Desk Reference (PDR). In managing overdosage, consider the possibility of multiple drug overdoses, interaction among drugs, and unusual drug kinetics in your patient.
Protect the patient’s airway and support ventilation and perfusion. Meticulously monitor vital signs, blood gases, blood chemistry values, and other variables.
If convulsions occur, consider diazepam, phenytoin, or phenobarbital. If the seizures are refractory, general anesthesia with thiopental or halothane and paralysis with a neuromuscular blocking agent may be necessary.
For hypotension, consider intravenous fluids, elevation of the legs, and an inotropic vasopressor, such as dopamine or norepinephrine (levarterenol). Theoretically, calcium gluconate may be helpful in treating some of the toxic cardiovascular effects of papaverine; monitor the ECG and plasma calcium concentrations.
Forced diuresis, peritoneal dialysis, hemodialysis, or charcoal hemoperfusion have not been established as beneficial for an overdose of Androskat (Papaverine Hydrochloride).
DOSAGE AND ADMINISTRATION
Androskat (Papaverine Hydrochloride) may be administered intravenously or intramuscularly. The intravenous route is recommended when an immediate effect is desired, but the drug must be injected slowly over the course of 1 or 2 minutes to avoid uncomfortable or alarming side effects.
Parenteral administration of Androskat (Papaverine Hydrochloride) in doses of 1 to 4 mL is repeated every 3 hours as indicated. In the treatment of cardiac extrasystoles, 2 doses may be given 10 minutes apart.
Androskat (Papaverine Hydrochloride) Injection, USP, 30 mg/mL
0517-4002-25 2 mL Vial packaged in boxes of 25
0517-4010-01 10 mL Multiple Dose Vial* packaged individually
*The 10 mL Multiple Dose Vial contains chlorobutanol 0.5% as a preservative.
Store at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F).
PROTECT FROM LIGHT. RETAIN IN CARTON UNTIL TIME OF USE.
SHIRLEY, NY 11967
Androskat (Phentolamine Mesylate) for Injection, USP is an antihypertensive, available in vials for intravenous and intramuscular administration. Each vial contains Androskat (Phentolamine Mesylate), USP, 5 mg, and mannitol USP, 25 mg, in sterile, lyophilized form.
Androskat (Phentolamine Mesylate), USP is 4,5-dihydro-2-[N-(m-hydroxyphenyl)-N-(p-methylphenyl) amino methyl]-1H- imidazole 1:1 methanesulfonate, and its structural formula is
Androskat (Phentolamine Mesylate), USP is a white or off-white, odorless crystalline powder with a molecular weight of 377.46. Its solutions are acid to litmus. It is freely soluble in water and in alcohol, and slightly soluble in chloroform. It melts at about 178°C.
Androskat (Phentolamine Mesylate) for Injection, USP produces an alpha-adrenergic block of relatively short duration. It also has direct, but less marked, positive inotropic and chronotropic effects on cardiac muscle and vasodilator effects on vascular smooth muscle.
Androskat (Phentolamine Mesylate) for Injection, USP has a half-life in the blood of 19 minutes following intravenous administration. Approximately 13% of a single intravenous dose appears in the urine as unchanged drug.
INDICATIONS AND USAGE
Androskat (Phentolamine Mesylate) for Injection, USP is indicated for the prevention or control of hypertensive episodes that may occur in a patient with pheochromocytoma as a result of stress or manipulation during preoperative preparation and surgical excision.
Androskat (Phentolamine Mesylate) for Injection, USP is indicated for the prevention or treatment of dermal necrosis and sloughing following intravenous administration or extravasation of norepinephrine.
Androskat (Phentolamine Mesylate) for Injection, USP is also indicated for the diagnosis of pheochromocytoma by the Androskat (Phentolamine Mesylate) for Injection, USP blocking test.
Myocardial infarction, history of myocardial infarction, coronary insufficiency, angina or other evidence suggestive of coronary artery disease; hypersensitivity to phentolamine or related compounds.
Myocardial infarction, cerebrovascular spasm, and cerebrovascular occlusion have been reported to occur following the administration of Androskat (Phentolamine Mesylate) for Injection, USP, usually in association with marked hypotensive episodes.
For screening tests in patients with hypertension, the generally available urinary assay of catecholamines or other biochemical assays have largely replaced the Androskat (Phentolamine Mesylate) for Injection, USP and other pharmacological tests for reasons of accuracy and safety. None of the chemical or pharmacological tests is infallible in the diagnosis of pheochromocytoma. The Androskat (Phentolamine Mesylate) for Injection, USP blocking test is not the procedure of choice and should be reserved for cases in which additional confirmatory evidence is necessary and the relative risks involved in conducting the test have been considered.
Tachycardia and cardiac arrhythmias may occur with the use of Androskat for Injection, USP or other alpha-adrenergic blocking agents. When possible, administration of cardiac glycosides should be deferred until cardiac rhythm returns to normal.
See DOSAGE AND ADMINISTRATION, Diagnosis of pheochromocytoma, Preparation .
Carcinogenesis, Mutagenesis, Impairment of Fertility
Long-term carcinogenicity studies, mutagenicity studies, and fertility studies have not been conducted with Androskat for Injection, USP.
Pregnancy Category C
Administration of Androskat (Phentolamine Mesylate) for Injection, USP to pregnant rats and mice at oral doses 24-30 times the usual daily human dose (based on a 60-kg human) resulted in slightly decreased growth and slight skeletal immaturity of the fetuses. Immaturity was manifested by increased incidence of incomplete or unossified calcanei and phalangeal nuclei of the hind limb and of incompletely ossified sternebrae. At oral doses 60 times the usual daily human dose (based on a 60-kg human), a slightly lower rate of implantation was found in the rat. Androskat (Phentolamine Mesylate) for Injection, USP did not affect embryonic or fetal development in the rabbit at oral doses 20 times the usual daily human dose (based on a 60-kg human). No teratogenic or embryo toxic effects were observed in the rat, mouse, or rabbit studies.
There are no adequate and well-controlled studies in pregnant women. Androskat (Phentolamine Mesylate) for Injection, USP should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from Androskat for Injection, USP, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
See DOSAGE AND ADMINISTRATION
Acute and prolonged hypotensive episodes, tachycardia, and cardiac arrhythmias have been reported. In addition, weakness, dizziness, flushing, orthostatic hypotension, nasal stuffiness, nausea, vomiting, and diarrhea may occur.
To report SUSPECTED ADVERSE REACTIONS, contact Precision Dose Inc. at 1-844-668-3942 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
No deaths due to acute poisoning with Androskat for Injection, USP have been reported.
Oral LD50’s (mg/kg): mice, 1000; rats, 1250.
Signs and Symptoms
Overdosage with Androskat (Phentolamine Mesylate) for Injection, USP is characterized chiefly by cardiovascular disturbances, such as arrhythmias, tachycardia, hypotension, and possibly shock. In addition, the following might occur: excitation, headache, sweating, pupillary contraction, visual disturbances; nausea, vomiting, diarrhea; hypoglycemia.
There is no specific antidote.
A decrease in blood pressure to dangerous levels or other evidence of shock like conditions should be treated vigorously and promptly. The patient’s legs should be kept raised and a plasma expander should be administered. If necessary, intravenous infusion of norepinephrine, titrated to maintain blood pressure at the normotensive level, and all available supportive measures should be included. Epinephrine should not be used, since it may cause a paradoxical reduction in blood pressure.
DOSAGE AND ADMINISTRATION
The reconstituted solution should be used upon preparation and should not be stored.
Note: Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.
1. Prevention or control of hypertensive episodes in the patient with pheochromocytoma.
For preoperative reduction of elevated blood pressure, 5 mg of Androskat for Injection, USP (1mg for children) is injected intravenously or intramuscularly 1 or 2 hours before surgery, and repeated if necessary.
During surgery, Androskat (Phentolamine Mesylate) for Injection, USP (5 mg for adults, 1 mg for children) is administered intravenously as indicated, to help prevent or control paroxysms of hypertension, tachycardia, respiratory depression, convulsions, or other effects of epinephrine intoxication. (Postoperatively, norepinephrine may be given to control the hypotension that commonly follows complete removal of a pheochromocytoma.)
2. Prevention or treatment of dermal necrosis and sloughing following intravenous administration or extravasation of norepinephrine.
For Prevention: 10 mg of Androskat (Phentolamine Mesylate) for Injection, USP is added to each liter of solution containing norepinephrine. The pressor effect of norepinephrine is not affected.
For Treatment: 5-10 mg of Androskat (Phentolamine Mesylate) for Injection, USP in 10 mL of saline is injected into the area of extravasation within 12 hours.
3. Diagnosis of pheochromocytoma - Androskat for Injection, USP blocking test.
The test is most reliable in detecting pheochromocytoma in patients with sustained hypertension and least reliable in those with paroxysmal hypertension. False-positive tests may occur in patients with hypertension without pheochromocytoma.
The CONTRAINDICATIONS, WARNINGS, and PRECAUTIONS sections should be reviewed. Sedatives, analgesics, and all other medications except those that might be deemed essential are withheld for at least 24 hours, and preferably 48 -72 hours, prior to the test. Antihypertensive drugs are withheld until blood pressure returns to the untreated, hypertensive level. This test is not performed on a patient who is normotensive.
The patient is kept at rest in the supine position throughout the test, preferably in a quiet, darkened room. Injection of Androskat (Phentolamine Mesylate) for Injection, USP is delayed until blood pressure is stabilized, as evidenced by blood pressure readings taken every 10 minutes for at least 30 minutes.
Five milligrams of Androskat (Phentolamine Mesylate) for Injection, USP is dissolved in 1mL of Sterile Water for Injection. The dose for adults is 5 mg; for children, 1 mg.
The syringe needle is inserted into the vein, and injection is delayed until pressor response to venipuncture has subsided.
Androskat (Phentolamine Mesylate) for Injection, USP is injected rapidly. Blood pressure is recorded immediately after injection, at 30-second intervals for the first 3 minutes, and at 60-second intervals for the next 7 minutes.
A positive response, suggestive of pheochromocytoma, is indicated when the blood pressure is reduced more than 35 mmHg systolic and 25 mmHg diastolic. A typical positive response is a reduction in pressure of 60 mmHg systolic and 25 mmHg diastolic. Usually, maximal effect is evident within 2 minutes after injection. A return to preinjection pressure commonly occurs within 15-30 minutes but may occur more rapidly.
If blood pressure decreases to a dangerous level, the patient should be treated as outlined under OVERDOSAGE.
A positive response should always be confirmed by other diagnostic procedures, preferably by measurement of urinary catecholamines or their metabolites.
A negative response is indicated when the blood pressure is elevated, unchanged, or reduced less than 35 mmHg, systolic and 25 mmHg diastolic after injection of Androskat for Injection, USP. A negative response to this test does not exclude the diagnosis of pheochromocytoma, especially in patients with paroxysmal hypertension in whom the incidence of false-negative responses is high.
If the intramuscular test for pheochromocytoma is preferred, preparation is the same as for the intravenous test. Five milligrams of Androskat (Phentolamine Mesylate) for Injection, USP is then dissolved in 1mL of Sterile Water for Injection. The dose for adults is 5 mg intramuscularly; for children, 3 mg. Blood pressure is recorded every 5 minutes for 30-45 minutes following injection. A positive response is indicated when the blood pressure is reduced 35 mmHg systolic and 25 mmHg diastolic, or more, within 20 minutes following injection.
Vials-each containing 5 mg of Androskat (Phentolamine Mesylate), USP, and 25 mg of mannitol, USP, in sterile, lyophilized form.
Cartons of 1….NDC 68094-101-20
The reconstituted solution should be used upon preparation and should not be stored.
Store at 20˚ to 25˚ C (68° - 77˚ F) with excursions between 15˚ to 30˚ C (59˚ to 86˚ F) [USP controlled Room Temperature]
You can also call Precision Dose Inc. at 1-800-397-9228 or visit www.precisiondose.com.
Precision Dose, Inc.
South Beloit, IL 61080
Androskat pharmaceutical active ingredients containing related brand and generic drugs:
Active ingredient is the part of the drug or medicine which is biologically active. This portion of the drug is responsible for the main action of the drug which is intended to cure or reduce the symptom or disease. The other portions of the drug which are inactive are called excipients; there role is to act as vehicle or binder. In contrast to active ingredient, the inactive ingredient's role is not significant in the cure or treatment of the disease. There can be one or more active ingredients in a drug.
Androskat available forms, composition, doses:
Form of the medicine is the form in which the medicine is marketed in the market, for example, a medicine X can be in the form of capsule or the form of chewable tablet or the form of tablet. Sometimes same medicine can be available as injection form. Each medicine cannot be in all forms but can be marketed in 1, 2, or 3 forms which the pharmaceutical company decided based on various background research results.
Composition is the list of ingredients which combinedly form a medicine. Both active ingredients and inactive ingredients form the composition. The active ingredient gives the desired therapeutic effect whereas the inactive ingredient helps in making the medicine stable.
Doses are various strengths of the medicine like 10mg, 20mg, 30mg and so on. Each medicine comes in various doses which is decided by the manufacturer, that is, pharmaceutical company. The dose is decided on the severity of the symptom or disease.
Androskat destination | category:
Destination is defined as the organism to which the drug or medicine is targeted. For most of the drugs what we discuss, human is the drug destination.
Drug category can be defined as major classification of the drug. For example, an antihistaminic or an antipyretic or anti anginal or pain killer, anti-inflammatory or so.
Androskat Anatomical Therapeutic Chemical codes:
A medicine is classified depending on the organ or system it acts [Anatomical], based on what result it gives on what disease, symptom [Therapeutical], based on chemical composition [Chemical]. It is called as ATC code. The code is based on Active ingredients of the medicine. A medicine can have different codes as sometimes it acts on different organs for different indications. Same way, different brands with same active ingredients and same indications can have same ATC code.
Androskat pharmaceutical companies:
Pharmaceutical companies are drug manufacturing companies that help in complete development of the drug from the background research to formation, clinical trials, release of the drug into the market and marketing of the drug.
Researchers are the persons who are responsible for the scientific research and is responsible for all the background clinical trials that resulted in the development of the drug.
Frequently asked QuestionsCan i drive or operate heavy machine after consuming Androskat?
Depending on the reaction of the Androskat after taken, if you are feeling dizziness, drowsiness or any weakness as a reaction on your body, Then consider Androskat not safe to drive or operate heavy machine after consumption. Meaning that, do not drive or operate heavy duty machines after taking the capsule if the capsule has a strange reaction on your body like dizziness, drowsiness. As prescribed by a pharmacist, it is dangerous to take alcohol while taking medicines as it exposed patients to drowsiness and health risk. Please take note of such effect most especially when taking Primosa capsule. It's advisable to consult your doctor on time for a proper recommendation and medical consultations.Is Androskat addictive or habit forming?
Medicines are not designed with the mind of creating an addiction or abuse on the health of the users. Addictive Medicine is categorically called Controlled substances by the government. For instance, Schedule H or X in India and schedule II-V in the US are controlled substances.
Please consult the medicine instruction manual on how to use and ensure it is not a controlled substance.In conclusion, self medication is a killer to your health. Consult your doctor for a proper prescription, recommendation, and guidiance.
Reviewsdrugs.com conducted a study on Androskat, and the result of the survey is set out below. It is noteworthy that the product of the survey is based on the perception and impressions of the visitors of the website as well as the views of Androskat consumers. We, as a result of this, advice that you do not base your therapeutic or medical decisions on this result, but rather consult your certified medical experts for their recommendations.
Visitor reported usefulNo survey data has been collected yet
One visitor reported side effectsDid you get side effects while taking the Androskat drug, or were there no side effects?
According to the survey conducted by website sdrugs.com users, the below-mentioned percentages indicate the number of people experiencing the side effects and the number of people not experiencing the side effects when taking Androskat medicine. Every drug produces minimal side effects, and they are negligible most times, when compared to the desired effect [use] of the medicine. Side effects depend on the dose you are taking, any drug interactions that happen when you are on other medications, if the patient is sensitive, and other associated conditions. If you cannot tolerate the side effects, consult your doctor immediately, so he can either adjust the dose or change the medication.
One visitor reported price estimatesWhat is your opinion about drug cost? Did you feel the cost is apt, or did you feel it is expensive?
The report given by the sdrugs.com website users shows the following figures about several people who felt the medicine Androskat is expensive, and the medicine is not expensive. The results are mixed. The perception of the cost of the medicine to be expensive or not depends on the brand name of the medicine, country, and place where it is sold, and the affordability of the patient. You can choose a generic drug in the place of the branded drug to save the cost. The efficiency of the medicine will not vary if it is generic or a branded one.
Visitor reported frequency of useNo survey data has been collected yet
Two visitors reported dosesWhat is the dose of Androskat drug you are taking?
According to the survey conducted among sdrugs.com website users, the maximum number of people are using the following dose 11-50mg. Few medications come in only one or two doses. Few are specific for adult dose and child dose. The dose of the medicine given to the patient depends on the severity of the symptom/disease. There can be dose adjustments made by the doctor, based on the progression of the disease. Follow-up is important.
One visitor reported time for resultsWhat is the time duration Androskat drug must be taken for it to be effective or for it to reduce the symptoms?
Most chronic conditions need at least some time so the dose and the drug action gets adjusted to the body to get the desired effect. The stastistics say sdrugs.com website users needed 1 day to notice the result from using Androskat drug. The time needed to show improvement in health condition after using the medicine Androskat need not be same for all the users. It varies based on other factors.
Visitor reported administrationNo survey data has been collected yet
Seven visitors reported age
The information was verified by Dr. Arunabha Ray, MD Pharmacology