Selective serotonin and norepinephrine reuptake inhibitors & drug with mixed actions

Question 1

list the SSNRI & mention other catergories (atypical &mixed)

Answer 1

1. venlafaxine
2. duloxetine
   - -> SSNRIs
3. reboxetine
   - ->SNRIs
4. bupropion
5. tianeptine
6. trazodone
7. nefazodone
8. vilazodone
9. mirtazapine
10. mianserine
    - ->mixed

SSNRIs act like TCA but they lack the TCA side effects.

Question 2

Name two drugs that block both NET and SERT

Answer 2

1. venlafaxine: in LOW dose it inhibits only SERT= SSRI (but you don’t have to wait for the elimination time like in SSRI so it’s a commonly used drug)
   in HIGH dose it inhibits both NET &SERT =TCA
   5-11 hr 1/2life (2x/day)

–> so good because you don’t need to change the drugs but only change the dose!!

2.duloxetine: SERT=NET

Question 3

Name one drug that only blocks NET

Answer 3

Reboxetine

• has a weak anticholinergic effect (blocks M receptors)
• can cause sleeping disturbances due to high levels of NE

Question 4

Name one drug that blocks both NET and DAT and mention it’s indications

Answer 4

Bupropion

• blocks DAT weakly and NET
• has a short duration so must be taken x2/day

indications:

1. stupor (immobilised) depression, the increased DA may improve it.
2. smoking cessation,decreases nicotine craving again due to increased DA
   - but has epileptic seizures as a side effect.

Question 5

name a drug used in depression that enhances SE uptake

Answer 5

Tianeptine

• the mechanism is not known for depression but may be due to the re-equilibration of the SE and NE proportions.
• has an anxiolytic effect so it is also used in alcoholics during withdrawal to decrease anxiety.

Question 6

mixed antidep:

name 3 drugs that not only block SERT but also affect the serotonin receptors. mention their indications

Answer 6

Trazodone &Nefazodone:
block SERT, have an ATG effect on 5HT2a & a1
indication: depression with insomnia( they have a strong sedative effect)

note –>trazodone: strongly associated with cardiac arrythmias & priapism–> due to a1 blockage

Vilazodone:
blocks SERT and is PA for 5HT1a
indication: depression with anxiety
-strong anxiolytic so no need for it to be combined with other drugs( antidepressant and anxiolytic drugs usually need to be combined)
side effect: GI so you increase the dose gradually and take it after a meal.

Question 7

mixed antidep:

name a2 antagonists ( also 5-HT2& 3 ATG)

Answer 7

1. mirtazapine-more commonly used
2. mianserine

a2R ATG:
Increased NE in the synaptic cleft

5-HT2c ATG:
–> anxiolytic and sedative effects, no modulation of libido, weight gain (SE causes anxiety and mioma)
–> can be used as antidepressant for people with anorexia
–> AGOMELATINE same but MT1 &2 agonist also
5-HT3 ATG:
–>antiemetic effects (SE causes GI side effects)

H1 ATG:
TCA side effects only on H1–> drowsiness & sedation
(no ATG effect on a1 & M)