Pharmacology Flashcards
Venlafaxine mechanism
SNRI
Duloxetine mechanism
SNRI + weak inhibitor of dopamine re-uptake
Reboxetine mechanism
NaRI (Noradrenalin reuptake inhibitor)
Mirtazepine class and mechanism
NaSSA (noradrenaline and serotonin specific antidepressant).
5HT2 antagonist, 5HT3 antagonist, H1 antagonist, alpha-1 & alpha-2 antagonist, moderate muscarinic antagonist
St John’s Wort mechanism
Weak MAOI and weak SNRI (also considered by some to be a weak SSRI)
Trazodone mechanism
Weak SRI and 5HT antagonist
Moclobemide mechanism
Reversible inhibitor of monoamine oxidase type A
Agomelatine mechanism
Melatonergic agonist (MT1 and MT2 receptors) and 5-HT2C antagonist
Donepezil mechanism
Reversible acetylcholinesterase inhibitor
Rivastigmine
Reversible acetylcholinesterase inhibitor and butyrylcholinesterase inhibitor
Galantamine
Reversible acetylcholinesterase inhibitor and binds allosterically to the nicotinic acetylcholine receptor
Tacrine
Reversible acetylcholinesterase inhibitor
Memantine
NMDA antagonist
Valproate
GABA agonist and NMDA antagonist
Gabapentin
GABA agonist
Topiramate
GABA agonist, NMDA antagonist, and Na channel stabiliser
Carbamazepine
Stabilises Na channels
Phenytoin
Stabilises Na channels
Lamotrigine
NMDA antagonist and stabilises Na channels
Pregabalin
Potent ligand for the alpha-2-delta subunit of voltage-gated calcium channels in the central nervous system
Benzodiazepines
GABA-A agonists
Z-drugs
GABA-A agonists
Buspirone
5HT1A partial agonist
Amisulpride mechanism and class
Substituted benzamide
D2/D3 selective antagonist (low affinity selective antagonist of ‘D2 like’ receptors (D2=D3>D4) it has little affinity for D1 like’ receptors (D1 and D5) or non dopaminergic receptors (serotonin, histamine, adrenergic, and cholinergic)
Olanzapine mechanism and class
Thienobenzodiazepines
Dopamine and 5HT2 antagonism
Aripiprazole mechanism and class
Arylpiperidylindole (quinolone)
Partial agonist at 5HT1A and D2, and 5HT2A antagonist
Clozapine mechanism and class
Dibenzodiazepines
High affinity for D4, (to a lesser extent D1, D2, D3, D5) also 5 HT 1A partial agonist and 5HT2 antagonist
Ketamine
NMDA antagonist
Phencyclidine
NMDA antagonist
Lofexedine
Alpha 2 agonist
Clonidine
Alpha 2 agonist
Buprenorphine
Partial agonist at the mu-opioid receptor
Naloxone
Pure opioid antagonist (will reverse mu, delta, and kappa)
Atomoxetine
Noradrenaline reuptake inhibitor
Varenicline
(Champix)Nicotinic receptor partial agonist
Bupropion
(Zyban) Norepinephrine-dopamine reuptake inhibitor, and nicotinic acetylcholine receptor antagonist
Disulfiram
Binds irreversibly to aldehyde dehydrogenase
Acamprosate
Metabotropic glutamate receptor antagonist and GABA-A agonist
Selegiline
selective, irreversible inhibition of monoamine oxidase type B (also inhibits MAO-A at higher doses
Immunologic adverse drug reactions Type I
Type I reactions
These arise when a drug-IgE complex binds to mast cells with a release of histamine and other inflammatory mediators. They characteristically cause anaphylaxis, urticaria, and bronchospasm. They generally occurs minutes to hours after exposure.
Immunologic adverse drug reactions Type II
Type II reactions
These occur when a IgG or IgM antibody binds to a cell which has been altered by a drug-hapten. They often manifest as blood abnormalities such as thromboctopenia and neutropenia. The timing of these reactions is variable.
Immunologic adverse drug reactions Type III
Type III reactions
These occur when drug-antibody complexes activate the complement system. They present with fever, rash, urticaria and vasculitis. These occur 1 to 3 weeks after exposure.
Immunologic adverse drug reactions Type IV
Type IV reactions
These arise when the MHC system presents drug molecules to T cells. They result in allergic contact dermatitis and rashes. They occur 2 to 7 days after cutaneous exposure.
Chlorpromazine class
Phenothiazines (Aliphatic side chain)
Pipothiazine
Phenothiazines (Piperidine side chain) (also includes Thioridazine)
fluphenazine
Phenothiazines (Piperizine side chain)
Trifluoperazine
Phenothiazines (Piperizine side chain)
Haloperidol
Butyrophenones
Flupenthixol
Thioxanthenes
zuclupenthixol
Thioxanthenes
Benzoxasoles
Risperidone
Dibenzothiazepines
Quetiapine
Serotonin receptors
- 5-HT3 is ligand gated
- 5-HT3 is most associated with nausea
- 5-HT7 is associated with circadian rhythms
- 5-HT2 stimulation is thought to underlie the effects of insomnia, agitation, and sexual dysfunction associated with SSRI use
Antidepressants for Nocturnal enuresis in children
Amitriptyline, Imipramine, Nortriptyline
Antidepressants for Phobic and obsessional states
Clomipramine
Antidepressants for Adjunctive treatment of cataplexy associated with narcolepsy
Clomipramine
Antidepressants for Panic disorder and agoraphobia
Citalopram, Escitalopram, Sertraline, Paroxetine, Venlafaxine
Antidepressants for Social anxiety/ phobia
Escitalopram, Paroxetine, Sertraline, Moclobemide, Venlafaxine
Antidepressants for Generalised anxiety disorder
Escitalopram, Paroxetine, Duloxetine, Venlafaxine
Antidepressants for OCD
Escitalopram, Fluoxetine, Fluvoxamine, Paroxetine, Sertraline
Antidepressants for Bulimia nervosa
Fluoxetine
Antidepressants for PTSD
Paroxetine, Sertraline
Which CYP450 shows the greatest phenotypic variation
CYP2D6
Which CYP450 is involved in clozapine metabolism
CYP1A2
Grapefruit juice inhibits which CYP450s
CYP3A4 and CYP1A2
Notable inducers of the CYP450 system
smoking, alcohol, barbiturates, carbamazepine, Phenytoin, and St John’s Wort
Notable inhibitors of the CYP450 system
chlorpromazine, SSRI’s, and grapefruit juice.
Illicit Drugs which interfere with ionotropic receptors or ion channels
Alcohol, nicotine, benzodiazepines, ketamine
Illicit Drugs which interfere with G coupled receptors
Opioids, cannabinoids, y-hydroxybutyrate (GHB)
Illicit Drugs that target monoamine transporters
Amphetamine, ecstasy, cocaine
Histamine H1 blockade casues
Weight gain, sedation
Alpha 1 blockade casues
Orthostatic hypotension, sedation, sexual dysfunction, priapism
Muscarinic central M1 blockade casues
Agitation, delirium, memory impairment, confusion, seizures
Muscarinic peripheral M1 blockade casues
Dry mouth, ataxia, blurred vision, narrow angle glaucoma, constipation, urinary retention, tachycardia
Mesolimbic pathway is responsible for which effect of antipsychotics
therapeutic benefit
Mesocortical pathway is responsible for which effect of antipsychotics
negative symptoms
Nigrostriatal pathway is responsible for which effect of antipsychotics
EPSEs
Tuberoinfundibular pathway is responsible for which effect of antipsychotics
hyperprotactinemia
Vitamin B1 =
thiamine
Vitamin B2 =
riboflavin
Vitamin B3 =
niacin
Vitamin B5 =
pantothenic acid
Vitamin B9 =
folic acid
Vitamin B12 =
cyanocobalamin