Doxapram

378.51

378.51

206-216-3

DTXSID2022963

R - Respiratory system

2934999090

32.8

3.6

Solid

1.1±0.1 g/cm3

217-219

536.4±50.0 °C at 760 mmHg

278.2±30.1 °C

1.562

H2O: Sparingly soluble

183.4 Ų [M+H]+ [CCS Type: TW, Method: Major Mix IMS/Tof Calibration Kit (Waters)]|185 Ų [M+H]+ [CCS Type: DT, Method: single field calibrated]

CRYSTALS FROM ISOPROPYL ETHER; BITTER TASTE; MP: 217-219 °C; SOL IN WATER; SPARINGLY SOL IN ALC; SLIGHTLY SOL IN CHLOROFORM /HYDROCHLORIDE/

STABLE IN LIGHT & IN AIR /HYDROCHLORIDE/

Intravenous LD50 values in the mouse and rat were approximately 75 mg/kg and in the cat and dog were 40 to 80 mg/kg. Symptoms of overdosage are extensions of the pharmacologic effects of the drug. Excessive pressor effect, tachycardia, skeletal muscle hyperactivity, and enhanced deep tendon reflexes may be early signs of overdosage.

For use as a temporary measure in hospitalized patients with acute respiratory insufficiency superimposed on chronic obstructive pulmonary disease.|FDA Label

Central Nervous System Stimulants; Respiratory System Agents|MEDICATION (VET): TO INCR VENTILATION & DECR SLEEPING TIME IN CATS & DOGS UNDER PENTOBARBITAL ANESTHESIA, & OCCASIONALLY IN ANESTHETIZED HORSES.|RESP CAN BE STIMULATED BY...DOSES THAT PRODUCE LITTLE GENERALIZED EXCITATION. DIRECT MEDULLARY STIMULATION IS LARGELY RESPONSIBLE FOR THIS EFFECT, BUT INDIRECT STIMULATION BY ACTIVATION OF PERIPHERAL CHEMORECEPTORS MAY... CONTRIBUTE. DURATION OF STIMULATION IS TRANSIENT AFTER SINGLE IV DOSE & SELDOM LASTS FOR...5-10 MIN.|DOXAPRAM...USED AS TEMPORARY MEASURES TO CORRECT ACUTE RESP INSUFFICIENCY IN PT WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE. INTERMITTENT OR CONTINUOUS INFUSION IS NECESSARY FOR SUSTAINED RESP STIMULATION & REDUCTION IN CARBON DIOXIDE TENSION...|For more Therapeutic Uses (Complete) data for DOXAPRAM (7 total), please visit the HSDB record page.

BECAUSE OF EFFECTIVENESS OF CONTROLLED VENTILATION & STANDARD SUPPORTIVE THERAPY IN TREATMENT OF VENTILATORY FAILURE, DOXAPRAM NORMALLY SHOULD NOT BE USED TO STIMULATE VENTILATION IN PT WITH DRUG-INDUCED COMA OR AN EXACERBATION OF CHRONIC LUNG DISEASES. /HYDROCHLORIDE/|DOXAPRAM IS CONTRAINDICATED IN PT WITH CONVULSIVE DISORDERS, HYPERTENSION, CEREBRAL EDEMA, HYPERTHYROIDISM, OR PHEOCHROMOCYTOMA & IN THOSE TAKING MONOAMINE OXIDASE INHIBITORS OR ADRENERGIC AGENTS. /HYDROCHLORIDE/

Doxapram is an analeptic agent (a stimulant of the central nervous system). The respiratory stimulant action is manifested by an increase in tidal volume associated with a slight increase in respiratory rate. A pressor response may result following doxapram administration. Provided there is no impairment of cardiac function, the pressor effect is more marked in hypovolemic than in normovolemic states. The pressor response is due to the improved cardiac output rather than peripheral vasoconstriction. Following doxapram administration, an increased release of catecholamines has been noted.

Drugs used for their effects on the respiratory system. (See all compounds classified as Respiratory System Agents.)|A loosely defined group of drugs that tend to increase behavioral alertness, agitation, or excitation. They work by a variety of mechanisms, but usually not by direct excitation of neurons. The many drugs that have such actions as side effects to their main therapeutic use are not included here. (See all compounds classified as Central Nervous System Stimulants.)

AFTER IV DOXAPRAM-HCL BOLUS INJECTIONS OR BRIEF INFUSIONS IN HEALTHY VOLUNTEER, PLASMA CONCN DECLINED IN MULTI-EXPONENTIAL FASHION. VOL OF DISTRIBUTION WAS 1.51 KG-1, & WHOLE BODY CLEARANCE WAS 370 ML MIN-1.|ENTERIC-COATED CAPSULES OF DOXAPRAM WERE ABSORBED RAPIDLY AFTER INITIAL DELAY, & SYSTEMIC AVAILABILITY WAS APPROX 60%. LESS THAN 5% OF AN IV DOSE WAS EXCRETED UNCHANGED IN URINE IN 24 HR.

DOXAPRAM YIELDS 4-(2-MORPHOLINOETHYL)-3,3-DIPHENYLPYRROLIDIN-2-ONE, & 1-ETHYL-4-(2-(3-OXOMORPHOLINO)ETHYL)-3,3-DIPHENYLPYRROLIDIN-2-ONE IN DOGS. PITTS, JE, BRUCE, RB, & FOREHAND, JB, XENOBIOTICA, 3, 73 (1973). /FROM TABLE/|AFTER IV DOXAPRAM-HCL BOLUS INJECTIONS OR BRIEF INFUSIONS IN HEALTHY VOLUNTEERS, A METABOLITE AHR 5955 WAS PRESENT IN PLASMA IN AMT COMPARABLE TO PARENT COMPD & HAD A SIMILAR HALF-LIFE.

AFTER IV DOXAPRAM-HCL BOLUS INJECTIONS OR BRIEF INFUSIONS IN HEALTHY VOLUNTEER, PLASMA CONCN DECLINED IN MULTI-EXPONENTIAL FASHION. HALF-LIFE FROM 4-12 HR WAS 3.4.

Doxapram produces respiratory stimulation mediated through the peripheral carotid chemoreceptors. It is thought to stimulate the carotid body by inhibiting certain potassium channels.|DOXAPRAM...STIMULATE ALL LEVELS OF CEREBROSPINAL AXIS. ADEQUATE DOSES PRODUCE TONIC-CLONIC CONVULSIONS SIMILAR IN PATTERN TO THOSE PRODUCED BY PENTYLENETETRAZOL. ...ACT BY ENHANCING EXCITATION RATHER THAN BY BLOCKING CENTRAL INHIBITION.

...SIDE EFFECTS INDICATIVE OF SUBCONVULSIVE CNS STIMULATION /ARE/... HYPERTENSION, TACHYCARDIA, ARRHYTHMIAS, COUGHING, SNEEZING, VOMITING, ITCHING, TREMORS, MUSCLE RIGIDITY, SWEATING, FLUSHING, & HYPERPYREXIA.

Docatone

SINGLE STAGE EXTRACTION, GAS-LIQ CHROMATOGRAPHY METHOD IS DESCRIBED FOR DETERMINING DOXAPRAM IN BLOOD PLASMA.

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