Antidepressants

Question 1

NE and and Specific Serotoninergic Antidepressants (NaSSA)

Answer 1

Mirtazapine

Presynaptic α2-adrenoceptor antagonist, 5HT2, 5HT3 antagonist, H1 receptor antagonist

Antidepressant, sedative effect
Major Depression

SE: Weight gain, sedation

Question 2

Anxiolytics BZD vs Barbiturates

Answer 2

BZD increases the ion channel opening frequencyBarbiturates, in turn, prolong the ion channel opening time

Question 3

BZD

Answer 3

Positive Allosteric modulators of the GABA A receptor complex
Non-selective binding to alpha subunits α1-5 enhances receptor affinity
Low dose sedative effect, high dose hypnotic

Question 4

Flumazenil

Answer 4

negative GABA modulator,which reduces GABA attachment

Question 5

Short acting BZD

Answer 5

Midazolam
T1 / 2 ~ 1.5-2.5 h i / v

Introductory anesthesia
Premedication prior to diagnostic or therapeutic manipulation
Seizures

Question 6

Alprazolam

Bromazepam

Answer 6

Anxiolytic, muscle relaxant, sedative, hypnotic action
NB! Unlike barbiturates, anxiolytic doses of BZD do not cause
very severe sedation, i.e. dose dependent effect(see proportional comparison of effects)

Panic attacks, anxiety
Stress symptomatic therapy

CI: Driving

Question 7

Problems of BZD therapy

Answer 7

1. Tolerance
2. Addiction
3. Rebound effect

Question 8

Non BZD, 2nd gen anxiolytics

Answer 8

Buspirone
Partial serotonin (5HT1A) receptor agonist
Lack of sedative function, habituation and addiction.

Although no interaction with alcohol has been found, nor driving is affected, individual patient response should be monitored at least at the start of therapy

Unlike BZD, the effects of B. develop much more slowly, within ~ 2 weeks
Anxiolytic effects

Generalized anxiety disorder

Question 9

Barbituric acid derivatives or barbiturates

Answer 9

Phenobarbital
1.Directly affects the chloride channel of the GABA A complex, acts as a GABA A receptor agonist
2. Acts as a GABA A positive allosteric modulator (binding site  subunit)
Barbiturates prolong GABA action
Dependence,addiction problem - barbituromania!

Cardiac neurosis, vegetative agitation
Sleep disorders
Epilepsy

IA: Induction of cytochrome CYP enzymes!

Question 10

BZD analog

Answer 10

Zolpidem
«Group Z»the chemical structure is different but the mechanism of action is similar to BZD
Selective association with the GABA A-α1 subunit
Importantly, not in all GABA -A complex-forming subunit variations
α1 subunits are involved
Unlike BZD - muscle relaxant and antiepileptic activity is minimal, risk of tolerance and addiction is minimal
Hypnotic effect (no anxiolytic effect)

For the short-term treatment of sleep disorders
SE: somnambulism, hallucinations

Question 11

Flumazenil

Answer 11

can prevent sedation caused by BZD and BZD analogues.
There is no antagonist for barbiturate intoxication.Use of BZD alone can rarely cause fatalities, but they contribute to another
CNS depressants such as alcohol