Analeptics : Analeptics Classification, PPT, Meaning

Analeptics : Analeptics Classification

Analeptics :

The analeptics are a group of potent and relatively nonselective CNS stimulants the convulsive dose of which lies near their analeptic dose. They once had Some employment as respiratory stimulants in countering the effects of CNS depressant drugs; however, they are now obsolete for that use. Some members of the group retain a very small therapeutic niche in the treatment of chronic obstructive pulmonary disease (COPD). Certain of the compounds have usefulness as pharmacologic tools and have interesting mechanism.

Picrotoxin :

Picrotoxin is obtained from the seeds of Anamirta cocculus. The active ingredient is picrotoxinin, with the following structure. 

 According to Jarboe,1 the encircled hydroxylactonyl moiety is mandatory for activity with the encircled 2-propenyl group assisting. Picrotoxin exerts its effects by interfering with the inhibitory effects of y-aminobutyric acid (GABA) at the level of the chloride channel (i.e., it is said to jam chloride channels). The drug is obsolete medically. Pharma- cologically it is used as an aid in determining how certain sedative-hypnotics and anticonvulsants act at the molecular level. 

Pentylenetetrazol :

Pentylenetetrazol. 6,7,8,9-Tetrahydro-5H-tet- razoloazepine; 1,5 pentamethylenetetrazole (Metrazol) has been used in conjunction with the electro- encephalograph to help locate epileptic foci. It is routinely used as a laboratory tool in determining potencies of potential anticonvulsant drugs in exper- imental animals. The drug may act as a convulsant by interfering with chloride conductance.2 Overall, it appears to share similar effects on chloride con- ductance with several other convulsive drugs, including picrotoxin.

Nikethamide. N,N-Diethylnicotinamide (Coramine) appears to act by facilitating excitatory processes rather than by depressing inhibitory ones. The overall effect resembles that of an amphetamine more than that of a drug such as picrotoxin.

It is possible to stimulate respiration with the drug without inducing generalized CNS stimulation. However, selectivity is still very low. The drug is obsolete in managing poisoning from sedative-hypnotic drugs. It may have a very limited place intreating acute respiratory insufficiency in COPD. It may also have value in correcting respiratory depression caused by oxygen therapy in COPD. 

Doxapram Hydrochloride, USP :

Doxapram Hydrochloride, USP. 1-Ethyl-4 (2-morpholinoethyl)-3,3-diphenyl-2-pyrrolidinone hydrochloride hydrate (Dopr├ám). Doxapram has CNS stimulant properties resembling those of nikethamide more than those of picrotoxin or pentylenetetrazol. It appears to have greater selectivity as a respiratory stimulant than nikethamide, but symptoms of generalized CNS stimulation are still frequent. Uses of doxapram are as described for nikethamide.

Category: respiratory stimulant

Usual dose range: IV, 1 to 15 mg/kg of body weight

Occurrence: Doxapram Hydrochloride Injection, USP

Analeptics  Analeptics Classification, PPT, Meaning Doxapram Hydrochloride

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