9 - ANXIOLYTIC DRUGS

Question 1

BENZODIAZEPINES (BZD) NAMES AND THE NAME OF AN ANTAGONIST

Answer 1

DIAZEPAM
OXAZEPAM
LORAZEPAM
NITRAZEPAM
BROMAZEPAM

FLUMAZENIL (I’ts used for treat BZD intoxications).

Question 2

MECHANISM OF ACTION OF BZD

Answer 2

They bind to the GABA A receptor in a different place than GABA They are allosteric modulators, that increase the affinity of GABA for the receptor, they modulate the opening of the receptor as they increase their opening frequency. A higher entrance of Cl in the cell is going to produce hyperpolarization in neurons; neural inhibiton.

Question 3

ACTIVATION OF THE ALPHA 1 SUBUNITS

Answer 3

SEDATIVE, ADDICTION, ANTICONVULSANT AND ANTEROGRADE AMNESIA EFFECTS

Question 4

ACTIVATION OF THE ALPHA 2 SUBUNITS

Answer 4

ANXIOLYTIC, ANTIDEPRESSIVE, ANTIHYPERAGESIA AND MYORELAXANT EFFECTS.

Question 5

INVERSE AGONISTS AND ANTAGONISTS

Answer 5

FLUMAZENIL IS AN EXAMPLE OF ANTAGONIST, IT IS USED TO TREAT INTOXICATIONS OF BZD (MAINLY THOSE PRODUCING RESPIRATORY CENTRE DEPRESSION). IT BLOCKS THE BINDING SITE OF BZD AND BLOCKS THE ACTIVATION OF THE RECEPTOR.

AS INVERSE AGONISTS, WE FIND B-CARBOLINES . GABA A RECEPTOR HAS TWO CONFORMATIONAL STATES, THE ONE IN WHICH AGONISTS CAN BIN D AND THE ONE IN WHICH PARTIAL AGONISTS CAN BIND . B-CARBOLINES BIND TO THE SECOND CONFORMATIONAL

Question 6

PHARMACOLOGICAL EFFECTS

Answer 6

RETARDATION OF ANXIETY AND AGGRESSIVENESS
SEDATION AND SLEEP INDUCTION
REDUCTION OF THE MUSCLE TONE
ANTEROGRADE AMNESIA; MUST BE AVOIDED IN ELDERLY
ANTICONVULSANT ACTIVITY; DIAZEPAM AND CLONAZEPAM