Methoxamine hydrochloride

247.72

247.09800

200-499-7

757102

DTXSID7045782

COLORLESS OR WHITE PLATE-LIKE CRYSTALS OR WHITE CRYSTALLINE POWDER|Crystals

64.71000

2.58670

212-216 °C

368.4ºC at 760 mmHg

176.6ºC

1.5204

>37.2 [ug/mL]

2-8°C

ODORLESS OR SLIGHT ODOR

pH of aq soln between 4.5 and 5.5

pKa= 9.2 @ 25 °C

149 Ų [M+H-H2O]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]|143.5 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

NONH for all modes of transport

3

DN4025000

METHOXAMINE HYDROCHLORIDE & INJECTIONS CONTAINING DRUG ARE THERMOSTABLE BUT SENSITIVE TO LIGHT

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).

...METHOXAMINE MAY PRODUCE CARDIAC ARRHYTHMIAS WHEN USED WITH GENERAL ANESTHETIC AGENTS. /METHOXAMINE/|METHOXAMINE HYDROCHLORIDE HAS BEEN TESTED AS 2% EYEDROPS ON THE THYROTOXIC PATIENTS & FOUND TO CAUSE MYDRIASIS & WIDENING OF THE PALPEBRAL FISSURE. THIS EFFECT HAS BEEN SHOWN TO BE POTENTIATED BY GUANETHIDINE.|WHEN VAGAL EFFECTS ARE BLOCKED BY ATROPINE, METHOXAMINE /HCL/ OFTEN SLOWS THE HEART SLIGHTLY. THIS IS PROBABLY DUE TO DIRECT ACTION ON ALPHA RECEPTORS. INJECTION OF THE DRUG INTO THE ARTERY LEADING TO THE SINUS NODE SLOWS THE HEART, AN EFFECT BLOCKED BY PHENTOLAMINE.|Concurrent use /with alpha-adrenergic-blocking agents such as: doxazosin, labetalol, phenoxybenzamine, phentolamine, prazosin, terazosin, tolazoline or with other medications with alpha-adrenergic blocking action, such as: haloperidol, loxapine, phenothiazines, thioxanthenes/ may antagonize the peripheral vasoconstriction of sympathomimetic agents; however, phentolamine may be used for therapeutic benefit. /Sympathomimetic agents/|For more Interactions (Complete) data for METHOXAMINE HYDROCHLORIDE (17 total), please visit the HSDB record page.

LD50 Mouse ip 92 mg/kg|LD50 Mouse iv 5030 ug/kg

Adrenergic alpha-Agonists; Sympathomimetics; Vasoconstrictor Agents|Methoxamine may be used intravenously in the treatment of hypotensive states or to relieve attacks of paroxysmal atrial tachycardia, particularly those associated with hypotension. /Methoxamine/|METHOXAMINE ... DOES NOT INCREASE VENTRICULAR RATE IN PATIENTS WITH HEART BLOCK. REFLEX BRADYCARDIA IS PROMINENT, &, THEREFORE, THE DRUG IS USED CLINICALLY TO RELIEVE ATTACKS OF PAROXYSMAL ATRIAL TACHYCARDIA. /METHOXAMINE/|THE DRUG IS USEFUL FOR THE TREATMENT OF HYPOTENSIVE STATES WHEN IT IS DESIRED TO RAISE BLOOD PRESSURE WITHOUT CARDIAC STIMULATION. HOWEVER, METHOXAMINE HAS VERY LITTLE EFFECT ON THE CAPACITANCE VEINS, SO THAT ITS USEFULNESS IS COMPROMISED, ESPECIALLY IN TREATMENT OF VARIOUS KINDS OF SHOCK.|For more Therapeutic Uses (Complete) data for METHOXAMINE HYDROCHLORIDE (9 total), please visit the HSDB record page.

Methoxamine should be used with caution in patients with hyperthyroidism, bradycardia, partial heart block, myocardial disease, or severe arteriosclerosis. Caution should be used to avoid overdosage of methoxamine, since it may cause undesirable hypertension and/or bradycardia.|Methoxamine can cause ventricular ectopic beats or severe bradycardia and decreased cardiac output. Decreased cardiac output may be especially harmful to geriatric patients and/or those with preexisting poor cerebral or coronary circulation. Bradycardia may be treated by administration of atropine. Methoxamine also increases cardiac work by increasing peripheral arterial resistance and may induce or exacerbate heart failure associated with a decreased myocardium. Some clinicians believe that the drug is contraindicated in shock caused by myocardial infarction. Large doses of methoxamine, especially if administered following repeated injections of the drug, may cause cardiac depression and a fall in blood pressure.|Methoxamine can cause severe peripheral and visceral vasoconstriction, reduced blood blow to vital organs, and decreased renal perfusion; reductions in glomerular filtration rate, urine output, and sodium excretion may occur as well as metabolic acidosis. These effects may be most likely to occur in hypovolemic patients. In addition, prolonged use of the drug may result in plasma volume depletion which may result in perpetuation of the shock state or the recurrence of hypotension when methoxamine is discontinued.|Methoxamine may cause restlessness, anxiety, nervousness, weakness, dizziness, precordial pain, tremor, respiratory distress, sweating, or pallor. Occasionally, injections of the drug may be followed by paresthesia in the extremities or feeling of coldness. A desire to void, a pilomotor response, and/or nausea and vomiting (often projectile) may also occur, especially with high doses. In addition, large doses of methoxamine may cause severe prolonged hypertension and severe headaches. Seizures and cerebral hemorrhage may result.|For more Drug Warnings (Complete) data for METHOXAMINE HYDROCHLORIDE (8 total), please visit the HSDB record page.

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.)|Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS. (See all compounds classified as Adrenergic alpha-1 Receptor Agonists.)

ITS PHARMACOLOGICAL PROPERTIES ARE ALMOST EXCLUSIVELY THOSE CHARACTERISTIC OF ALPHA-RECEPTOR STIMULATION, SINCE IT ACTS DIRECTLY AT THESE SITES. ... THE OUTSTANDING EFFECT IS AN INCREASE IN BLOOD PRESSURE DUE ENTIRELY TO VASOCONSTRICTION.|METHOXAMINE, GIVEN INTRAVENOUSLY OR INTRAMUSCULARLY IN MAN, CAUSES A RISE IN SYSTOLIC & DIASTOLIC BLOOD PRESSURES THAT PERSISTS FOR 60 TO 90 MINUTES. THE PRESSOR EFFECT IS DUE ALMOST EXCLUSIVELY TO AN INCREASE IN PERIPHERAL RESISTANCE. CARDIAC OUTPUT IS DECREASED OR UNCHANGED. /METHOXAMINE/|METHOXAMINE HAS A RELATIVELY SELECTIVE ACTION ON POSTSYNAPTIC COMPARED WITH PRESYNAPTIC RECEPTOR OF PULMONARY ARTERY; BOTH SYSTEMS WERE OF SIMILAR SENSITIVITY TO NOREPINEPHRINE & EPINEPHRINE.|TRITIUM-LABELED METHOXAMINE CROSSED THE BLOOD-BRAIN BARRIER IN RAT. THUS METHOXAMINE IS CENTRALLY ACTIVE ALPHA-ADRENERGIC AGONIST & CONCEPT THAT HYPOTHALAMIC ADRENERGIC MECHANISMS ARE INVOLVED IN ELECTROENCEPHALOGIC & BEHAVIORAL AROUSAL IS SUPPORTED.

METHOXAMINE HYDROCHLORIDE HAS BEEN TESTED AS 2% EYEDROPS ON THYROTOXIC PATIENTS & FOUND TO CAUSE MYDRIASIS & WIDENING OF THE PALPEBRAL FISSURE.|HIGH DOSES MAY PRODUCE DANGEROUS BLOOD PRESSURE ELEVATIONS & HEADACHE. URINARY URGENCY, TINGLING IN THE EXTREMITIES, & VOMITING MAY OCCUR. REFLEX BRADYCARDIA & POSSIBLE DEPRESSION OF CARDIAC OUTPUT LIMIT ITS APPLICATION TO NEUROVASCULAR SHOCK STATES INDUCED BY SPINAL ANESTHESIA.

Hydrochloride, Methoxamine

METHOXAMINE HYDROCHLORIDE, USP (VASOXYL), IS AVAILABLE AS A SOLUTION (10 OR 20 MG/ML) FOR INTRAMUSCULAR INJECTION. THE DOSE VARIES FROM 10 TO 20 MG. IV INJECTIONS OF 3 TO 5 MG MAY ALSO BE GIVEN WITH PRECAUTIONS PROPERLY ACCORDED TO IV INJECTIONS OF SYMPATHOMIMETIC AMINES.

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