Fichas
Anti-depressants
Fichas del conjunto (23)
- 1—Phenelzine
non selective MAO inhibitor
from Isoniazid
- 2—Moclobemide
MAO-A inhibitor
- 3—Tranylcypromine
non selective MAO inhibitor
- 4—Iproniazid
non selective MAO inhibitor
from Isoniazid
- 5—Doxepin
dibenzoxepine
tertiary TCA NSRI
Z>active than E for inhibiting reuptake of 5HT
N-demethylated doxepin is also selective inhibitor of NET
- 6—Amitriptyline
dibenzocyclohepten-5-ylidene
tertiary TCA NSRI
- 7—Imipramine
dihydrodibenzazepine
tertiary TCA NSRI
- 8—Trimipramine
tertiary TCA NSRI
dihydrodibenzazepine
branching decreases affinity by 100x for 5-HT and NE transporters
- 9—Clomipramine
tertiary TCA NSRI
substituting a halogen into 3- of dihydrodibenzazepine enhances affinity for SERT
- 10—(+) Venlafaxine
non tricyclic NSRI
metabolite: equipotent ODV
both have high affinity for 5-HT reuptake and weak inhibition of NE and DA reuptake
risk of cardiotoxicity
low binding to plasma proteins - 11—(+) Milnacipran
non tricyclic NSRI
inhibits 5-HT and NE reuptake
efficacy similar to TCAs and SSRIs with lower side effects
weak affinity for adrenergic, muscarinic and H1 receptors
inactive metabolites
- 12—Duloxetine
fluoxetine analogue
dual inhibition: SERT>NET
low affinity for other neuroreceptors-->low adverse effects
diabetic peripheral neuropathy
2 active metabolites
- 13—Desipramine
dihydrodibenzazepine
secondary amine TCA (SNRI)
more selective for NET
inactive metabolite 2-hydroxydesipramine
- 14—Protriptyline
dibenzocycloheptriene
secondary amine TCA (SNRI)
more selective for NET
- 15—Nortriptyline
dibenzocyclohepten-5-ylidene
secondary amine TCA (SNRI)
more selective for NET
- 16—Maprotiline
tetracyclic (bicyclic ring middle ring)
secondary amine TCA (SNRI)
more selective for NET
- 17Amoxapinetertiary amine TCA (SNRI)
structurally related to Loxapine
blocks DA
EPS
aromatic hydroxylation gives active metabolite - 18—Atomoxetine
non tricyclic SNRI
one active metabolite with CYP2D6
- 19—4-hydroxy-(R)-atomoxetine
active metabolite of atomoxetine
- 20—(S)-fluoxetine
phenoxyphenylalkylamine SSRI
less bulky than TCAs
demethylated active metabolite
both have long half lives
marketed as racemate (S more potent than R)
- 21—Paroxetine
phenoxyphenylalkylamine SSRI
potent and selective inhibitor of SERT and low affinity for NET and DAT
phenylpropylamine grp may be folded into piperidine in an analogue
inhibitor of CYP2D6
inactive metabolites
electronegative 4-substitution is necessary for selectivity and affinity for SERT
- 22—Citalopram
phenoxyphenylalkylamine SSRI (orally)
greatest selectivity for 5-HT reuptake inhibition compared to other SSRIs
(S):escitalopram-->27x >potent than R
active liver metabolite N-demethyl
less highly protein bound than other SSRIs-->less drug interactions
- 23—Sertraline
phenylalkylamine SSRI
potent and selective inhibitor of SERT reuptake
weak inhibitor of CYP3A4
N-desmethyl-sertraline is 5-10x less potent as inhibitor of 5-HT reuptake
orally active
Información
- Descripción
- Pharmacy Fichas sobre Anti-depressants, creado por Cyrielle Saba el 24/10/2020.
- Creado por
- Cyrielle Saba
- Visitas
- 11
- Valoración