17- A) PHENYLETHYLAMINES Flashcards
PHENYLETHYLAMINES
Alkaloids with a chemical structure closely related to that of the neurotransmitters adrenaline (epinephrine) and noradrenaline (norepinephrine), amphetamine and certain designer drugs.
NATURAL ALKALOIDS
EPHEDRINE
PSEUDOEPHEDRINE
CATHIONE
MESCALINE
EPHEDRINE AND PESUDOEPHEDRINE
-Basic nitrogen, secondary amine, non heterocyclic. -It does not give classic precipitation reactions of alkaloids. -Reaction for detection: ninhydrin (blue-violet).
PHENYLETHYLAMINE- CONTAINING DRUGS
Steam of Ephedra
Heart-leaf Sida; Flowering top and root of Sida cordifolia
Ephedra distachya
Ephedra equisetina
Several species of Ephedra are used as a source of ephedrine and pseudoephedrine, although they may also be obtained by easy synthesis.
Ephedras spp. contain about 0.5-2.0% of alkaloids.
Of them, ephedrine range from 30 to 90% according to the species.
PHARMACOLOGICAL ACTION OF EPHEDRINE AT THE PERIPHERAL LEVEL
• Indirect sympathomimetic. Inhibit reuptake of norepinephrine.
a) Cardiac stimulation: positive chronotropic and inotropic
effects, producing tachycardia.
b) Vessels: potent vasoconstriction. Increases systolic and
diastolic blood pressure.
c) Bronchodilatation
PHARMACOLOGICAL ACTION OF EPHEDRINE AT THE ON THE NERVOUS CENTRAL SYSTEM
•Ephedrine cross the blood-brain barrier, increasing levels of catecholamines. Its metabolism is slow so that it has long-life
action than the neurotransmitter epinephrine.
•Produces a stimulating psychic effect, increases concentration and reduces the sensation of fatigue, hunger and the need of sleep.
Side effects include anxiety, tremors and insomnia.
THERAPEUTIC INDICATIONS OF EPHEDRINE BY ITS VASOCONSTRICTOR EFFECT
- nasal decongestant (treatment of the acute congestion,
rhinitis, sinusitis and rhinopharyngitis). - prophylaxis and treatment of rhinopharynx infections (due
to their antiseptic and vasoconstrictive properties). - hemorrhoidal crisis (treatment of the painful symptoms of
the acute attack of piles.
It is often associated with: antihistamine, analgesics, local anesthetics,
antiseptics.
THERAPEUTIC INDICATIONS OF EPHEDRINE BY ITS BRONCHODILATOR EFFECT
- Due to its bronchodilator effect (hydrochloride or
sulphate) , it is also used in association with other drugs in: - non-productive coughs
- antiasthmatic
SPANISH PHARMACEUTICAL SPECIALITIES (EPHEDRINE -PSEUDO)
- Sandival (Pseudoephedrine)
- Hemoal (Ephedrine)
SANDIVAL
EPHEDRINE Treatment of symptoms of the common cold and influenza-like states: congestive, febrile and painful symptoms.
HEMOAL
EPHEDRINE Hemorrhoids, anal fissure. Symptomatic treatment of pain or itching associated with hemorrhoids or anal fissure.
KHAT, ABYSSINIAN TEA, LEAF OF CATHA EDULIS (INFORMATION)
Young and fresh leaves, constitute a masticatory drug (stimulatory effect) used like coca leaf to
suppress the depression and to combat the sensation of hunger and fatigue.
They contain (-) cathinone. It has pharmacological properties analogous to those of (+)- amphetamine, with simiar potency and mechanism of action.
Effects; aggressiveness, paranoia, personality disorders.
Cultivation, sale and illicit use are produced outside their countries of origin.
NATURAL ALKALOID WHICH IS COINTAINED IN CATHA EDULIS - ABYSSINIAN TEA
They contain (-) cathinone. It has pharmacological properties analogous to those of (+)- amphetamine, with simiar potency and mechanism of action.
EFFECTS OF CATHA EDULIS, ABYSSINIAN TEA
Effects; aggressiveness, paranoia, personality disorders.
PEYOTE, MESCAL; ECHINOCACTUS WILLIAMSII (INFORMATION)
Peyote is a potent hallucinogenic globular cactus. It is collected before the rainy season which precedes the flowering by cutting at ground level.
When dry, it acquires a dark grey colour, then known as “peyote button” or “mescal
button” (8-9% TA).