Metaraminol

167.21

167.21

818U2PZ2EH

DTXSID8023268

C - Cardiovascular system

66.5

0.6

Solid

1.198g/cm3

107.5 °C

218 °C

170.3ºC

1.4760 (estimate)

1.28e+01 g/L

Metaraminol bitartrate injection should be stored at room temperature and protected from light. Freezing and temperatures above 40 deg C should be avoided. /Metaraminol bitartrate/

8.79None

8.79

Crystals; MP: 176-177 °C; pH of 1% aq soln: about 3.5; freely sol in water /l-form Bitartrate/|PRACTICALLY ODORLESS /BITARTRATE/|Hygroscopic; Specific optical rotation: -19.75 deg @ 20 °C/D; freely sol in water /l-form hydrochloride/|Crystals; MP: 190 °C; specific optical rotation: -21.66 deg @ 20 °C/D; sol in water /l-form oxalate dihydrate/|WHITE CRYSTALLINE POWDER /BITARTRATE/

SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).

LD50=240 mg/kg (rat, oral); LD50=99 mg/kg (mouse, oral)

MAO INHIBITORS...HAVE THE POTENTIAL FOR DRUG INTERACTION WITH METARAMINOL THROUGH INHIBITION OF OXIDATIVE DEAMINATION OF SYMPATHOMIMETIC AMINES. THE RESULT MAY BE AN INCREASED TISSUE STORE OF NOREPINEPHRINE, WHICH WILL PRODUCE A HEIGHTENED HYPERTENSIVE RESPONSE SECONDARY TO THE INDIRECT ACTIONS OF METARAMINOL. /BITARTRATE/|GUANETHIDINE, RESERPINE, & METHYLDOPA AFFECT POSTGANGLIONIC NERVE ACTIVITY, EITHER BY DECREASING NOREPINEPHRINE STORES OR BY EFFECTING ITS RELEASE. THEREFORE, THESE DRUGS WILL INTERFERE WITH THE INDIRECT NOREPINEPHRINE-RELEASING ACTIONS OF METARAMINOL & MAY LIMIT ITS EFFICACY. /BITARTRATE/|CARDIAC OUTPUT INCREASES STRIKINGLY WHEN SLOWING OF THE HEART IS PREVENTED BY ATROPINE.|THE ANTIBACTERIAL ACTION OF FURAZOLIDONE IS ACCOMPANIED BY PROGRESSIVE & GENERALIZED INHIBITION OF MONOAMINE OXIDASE & THE CONCURRENT OR SUBSEQUENT ADMIN OF /METARAMINOL/...COULD RESULT IN A HYPERTENSIVE CRISIS. /BITARTRATE/|For more Interactions (Complete) data for METARAMINOL (20 total), please visit the HSDB record page.

LD50 Rat oral 240 mg/kg|LD50 Rat ip 41 mg/kg|LD50 Rat sc 117 mg/kg|LD50 Mouse oral 99 mg/kg|For more Non-Human Toxicity Values (Complete) data for METARAMINOL (6 total), please visit the HSDB record page.

Approximately 45%

For the treatment and prevention of hypotension due to hemorrhage, spinal anesthesia, and shock associated with brain damage

Adrenergic alpha-Agonists; Adrenergic Agents; Sympathomimetics; Vasoconstrictor Agents|MEDICATION (VET): /USED/ IN HYPOTENSIVE STATES IN DOGS AS MAY OCCUR IN ENDOTOXIC SHOCK OR BARBITURATE ANESTHESIA. /IT/ HAS BEEN USED WITH PHENYLEPHRINE OR AMPHETAMINE. PROBABLY INDICATED IN SHOCK ASSOCIATED WITH MYOCARDIAL INFARCTION.|...USED...IN CERTAIN ACUTE HYPOTENSIVE CONDITIONS SUCH AS ANAPHYLACTIC SHOCK (AFTER INITIAL MANAGEMENT WITH EPINEPHRINE) OR SHOCK SECONDARY TO MYOCARDIAL INFARCTION, TRAUMA, SEPTICEMIA, GRAM-NEGATIVE BACTERIAL ENDOTOXINS, & ADVERSE DRUG REACTIONS. /BITARTRATE/|... IS USED ALMOST EXCLUSIVELY FOR TREATMENT OF HYPOTENSIVE STATES. IT HAS BOTH DIRECT & INDIRECT ACTION & ITS OVERALL EFFECTS ARE SIMILAR TO THOSE OF NOREPINEPHRINE, BUT IT IS MUCH LESS POTENT & HAS A MORE PROLONGED ACTION. IT LACKS CNS STIMULANT EFFECTS.|For more Therapeutic Uses (Complete) data for METARAMINOL (12 total), please visit the HSDB record page.

VET: CONTINUED USE MAY DEPLETE NOREPINEPHRINE STORES.|IT IS NOT RECOMMENDED IN HYPOVOLEMIC SHOCK. /BITARTRATE/|...METARAMINOL CAN CAUSE SHOCK WHEN GIVEN BY PROLONGED INFUSION & SOME AUTHORITIES ARE RELUCTANT TO GIVE METARAMINOL...IN ANY KIND OF SHOCK OTHER THAN ANAPHYLAXIS. METARAMINOL CAN CAUSE A SLOUGH IF EXTRAVASATED. /BITARTRATE/|SUBCUTANEOUS INJECTIONS SHOULD BE AVOIDED SINCE TISSUE SLOUGHING MAY OCCUR.|For more Drug Warnings (Complete) data for METARAMINOL (14 total), please visit the HSDB record page.

Metaraminol is a potent sympathomimetic amine that increases both systolic and diastolic blood pressure. Metaraminol is indicated for prevention and treatment of the acute hypotensive state occurring with spinal anesthesia. It is also indicated as adjunctive treatment of hypotension due to hemorrhage, reactions to medications, surgical complications, and shock associated with brain damage due to trauma or tumor. Metaraminol acts on both α1-adrenergic receptors but appears to have no effect on β-adrenergic receptors. It acts by increasing the force of the heart's pumping action as well as constricting peripheral blood vessels.

Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS. (See all compounds classified as Adrenergic alpha-1 Receptor Agonists.)|Drugs that mimic the effects of stimulating postganglionic adrenergic sympathetic nerves. Included here are drugs that directly stimulate adrenergic receptors and drugs that act indirectly by provoking the release of adrenergic transmitters. (See all compounds classified as Sympathomimetics.)|Drugs used to cause constriction of the blood vessels. (See all compounds classified as Vasoconstrictor Agents.)

The effect starts 1-2 min after IV injection, 10 min after IM injection, 5-20 min after subcutaneous injection.|METARAMINOL IS ABSORBED AFTER ORAL ADMINISTRATION.|METARAMINOL WAS TAKEN UP BY THE RABBIT HEART IN MEASURABLE QUANTITIES FOR AT LEAST 8 DAYS FOLLOWING A SINGLE IV INJECTION. IT WAS EXTENSIVELY DISTRIBUTED IN HEART, LUNGS, LIVER, KIDNEYS, & SKELETAL MUSCLE & POORLY IN THE SPLEEN, BRAIN, FAT, & STOMACH.|EXCEPT FOR THE BRAIN, PERIPHERALLY ADMIN METARAMINOL WAS WELL DISTRIBUTED IN RATS. ORGANS WITH A LARGE POPULATION OF NOREPINEPHIRINE (NE) STORAGE VESICLES SUCH AS THE HEART, SPLEEN, & ADRENAL, TOOK UP RELATIVELY LARGE AMT & RETAINED IT LONGER THAN LIVER, LUNG & KIDNEY.|METARAMINOL IS ABSORBED AFTER ORAL ADMIN; HOWEVER, FOR EQUAL EFFECTS, ORAL DOSES MUST BE 5 OR 6 TIMES GREATER THAN DOSES GIVEN IM OR IV. THE PRESSOR EFFECT OF AN IM DOSE OF 5 MG LASTS FOR ABOUT 1.5 HOURS.

Hepatic|THE FACT THAT METARAMINOL, 1-(M-HYDROXYNOREPHEDRINE), REMAINED UNCHANGED & BOUND TO TISSUES FOR 1-2 WK AFTER INGESTION PROMPTED IN VITRO STUDIES, WHICH SHOWED THAT THE DRUG RESISTS BIOTRANSFORMATION BY LIVER ENZYMES WHICH METABOLIZE STRUCTURALLY RELATED COMPOUNDS. /MAMMAL SPECIES NOT LISTED IN SOURCE/

Metaraminol acts through peripheral vasoconstriction by acting as a pure alpha-1 adrenergic receptor agonist, consequently increasing systemic blood pressure (both systolic & diastolic). Its effect is thought to be associated with the inhibition of adenyl cyclase which leads to an inhibition of the production of cAMP. Another effect of Metaraminol is that it releases norepinephrine from its storage sites indirectly.|BY DIRECT ACTION ON ALPHA ADRENERGIC RECEPTORS & INDIRECT ACTION THROUGH THE RELEASE OF NOREPINEPHRINE FROM STORAGE SITES...PRODUCES VASOCONSTRICTION, INCREASED PERIPHERAL VASCULAR RESISTANCE, & A RESULTANT INCREASED BLOOD PRESSURE. REFLEX BRADYCARDIA USUALLY OCCURS &...RENAL & CEREBRAL BLOOD FLOW DECREASES. /BITARTRATE/|CARDIAC INOTROPY INCREASES, BUT LESS SO THAN WITH NOREPINEPHRINE & CARDIAC OUTPUT REMAINS UNCHANGED OR MAY SLIGHLY DECREASE IF BRADYCARDIA OCCURS. SOME BETA ADRENERGIC MEDIATED VASODILATION OCCURS WITH METARAMINOL, BUT ALPHA EFFECTS PREDOMINATE. /BITARTRATE/|FOLLOWING IV ADMIN OF 1.5 MG/KG TO RABBITS, THERE WAS A POSITIVE CORRELATION BETWEEN PLASMA DRUG LEVEL & ITS VASOPRESSOR EFFECT. DRUG IS APPARENTLY DIRECT-ACTING SYMPATHOMIMETIC AMINE & ITS ACTION IS PROBABLY TERMINATED BY ITS DILUTION IN BODY FLUIDS & TISSUE UPTAKE.

OVERDOSES...CAN CAUSE HYPERTENSIVE CRISES & CARDIAC TACHYARRHYTHMIAS. EVEN IN ABSENCE OF A HYPERTENSIVE EFFECT, PALLOR, TACHYCARDIA, PALPITATION, PRECORDIAL PAIN, WEAKNESS, DIZZINESS, TREMOR, RESPIRATORY DISTRESS, & ANXIETY CAN OCCUR. /BITARTRATE/|TACHYPHYLAXIS MAY DEVELOP AFTER PROLONGED ADMIN, PRESUMABLY SECONDARY TO NOREPHINEPHRINE DEPLETION FROM STORAGE SITES. A DECREASE IN PLASMA VOLUME MAY ALSO OCCUR AS POST-CAPILLARY VASOCONSTRICTION PRODUCES TRANSUDATION OF FLUID INTO EXTRACELLULAR SPACE. /BITARTRATE/|...SUBCUTANEOUS TISSUE NECROSIS OCCURS ONLY RARELY, BUT THE LONGER DURATION OF ACTION MAY BE HAZARDOUS IF OVERDOSAGE & UNINTENTIONAL HYPERTENSION OCCURS. FURTHERMORE, HYPOTENSION MAY RECUR AFTER PROLONGED USE, POSSIBLY SECONDARY TO NOREPINEPHRINE DEPLETION. /BITARTRATE/|Overdosage may result in severe hypertension, cerebral hemorrhage, convulsions, acute pulmonary edema, cardiac arrest, and/or arrhythmias. Headache may be a symptom of hypertension.

Aramine

METARAMINOL BITARTRATE USP (ARAMINE), IS AVAILABLE IN 1-ML AMPULS & 10-ML VIALS AS A STERILE SOLN (10 MG/ML) FOR INTRAMUSCULAR INJECTION, USUALLY IN DOSE OF 5-10 MG, OR, AFTER SUITABLE DILUTION, FOR IV INFUSION. RATE OF ADMIN IS REGULATED ACCORDING TO THE INDIVIDUAL'S RESPONSE TO THE DRUG. /BITARTRATE/

VET: MAY DISCOLOR POLYETHYLENE TUBING OR DEVICES.

SIMULTANEOUS DETERMINATION OF METARAMINOL BITARTRATE, METHYLPARABEN & PROPYLPARABEN IN INJECTABLE FORMULATIONS.

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients|Pharmaceuticals