17- A) PHENYLETHYLAMINES Flashcards

1
Q

PHENYLETHYLAMINES

A

Alkaloids with a chemical structure closely related to that of the neurotransmitters adrenaline (epinephrine) and noradrenaline (norepinephrine), amphetamine and certain designer drugs.

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2
Q

NATURAL ALKALOIDS

A

EPHEDRINE
PSEUDOEPHEDRINE
CATHIONE
MESCALINE

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3
Q

EPHEDRINE AND PESUDOEPHEDRINE

A
-Basic nitrogen, secondary amine,
non heterocyclic.
-It does not give classic precipitation
reactions of alkaloids.
-Reaction for detection: ninhydrin
(blue-violet).
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4
Q

PHENYLETHYLAMINE- CONTAINING DRUGS

A

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.

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5
Q

PHARMACOLOGICAL ACTION OF EPHEDRINE AT THE PERIPHERAL LEVEL

A

• 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

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6
Q

PHARMACOLOGICAL ACTION OF EPHEDRINE AT THE ON THE NERVOUS CENTRAL SYSTEM

A

•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.

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7
Q

THERAPEUTIC INDICATIONS OF EPHEDRINE BY ITS VASOCONSTRICTOR EFFECT

A
  • 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.
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8
Q

THERAPEUTIC INDICATIONS OF EPHEDRINE BY ITS BRONCHODILATOR EFFECT

A
  • Due to its bronchodilator effect (hydrochloride or
    sulphate) , it is also used in association with other drugs in:
  • non-productive coughs
  • antiasthmatic
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9
Q

SPANISH PHARMACEUTICAL SPECIALITIES (EPHEDRINE -PSEUDO)

A
  • Sandival (Pseudoephedrine)

- Hemoal (Ephedrine)

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10
Q

SANDIVAL

A
EPHEDRINE 
Treatment of symptoms of the
common cold and influenza-like
states: congestive, febrile and
painful symptoms.
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11
Q

HEMOAL

A
EPHEDRINE
Hemorrhoids, anal fissure.
Symptomatic treatment of pain
or itching associated with
hemorrhoids or anal fissure.
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12
Q

KHAT, ABYSSINIAN TEA, LEAF OF CATHA EDULIS (INFORMATION)

A

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.

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13
Q

NATURAL ALKALOID WHICH IS COINTAINED IN CATHA EDULIS - ABYSSINIAN TEA

A

They contain (-) cathinone. It has pharmacological properties analogous to those of (+)- amphetamine, with simiar potency and mechanism of action.

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14
Q

EFFECTS OF CATHA EDULIS, ABYSSINIAN TEA

A

Effects; aggressiveness, paranoia, personality disorders.

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15
Q

PEYOTE, MESCAL; ECHINOCACTUS WILLIAMSII (INFORMATION)

A

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).

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16
Q

MESCALINE

A

PEYOTE, MESCAL; ECHINOCACTUS WILLIAMSII

Mescaline:has clinical effects
similar to those of LSD (lysergic
acid diethylamide): psychic,
cognitive and physical.

17
Q

EFFECTS PRODUCED BY MESCALINE

A
The ingestion
produces a distortion
of the perception of
shapes, an
intensification of
colours, auditory
hallucinations, and a
slowing in the
perception of time.
The physical
symptoms include
mydriasis,
tachycardia,
bradypnea, nausea,
agitation and
anxiety. At high
doses, memory loss,
hypertensive
encephalopathy and
intracranial
hemorrhage.