CNS Stimulants (4)
- methylphenidate 2. dextroamphetamine 3. methamphetamine 4. phentermine
Mechanism of CNS Stimulants
-increase catecholamines at the synaptic cleft, esp. NE and DA.
Clincial use of CNS stimulants
ADHD Narcolepsy Appetite control
Antipsychotics (neuroleptics) (5)
- Haloperidol 2. Trifluoperazine 3. Fluphenazine 4. Thioridazine 5. Chlorpromazine
Mechanism of Antipsychotics
All typical antipsychotics block dopamine D2 receptors (increase cAMP).
Clinical use of antipsychotics
-schizophrenia (mainly + symptoms) -psychosis -acute mania -Tourette’s
Antipsychotics are very slow to be removed from the body because…
they are highly lipid soluble and are stored in body fat.
Toxicity of antipsychotics
-extrapyramidal system effects (dyskinesias) -endocrine side effects (galactorrhea) -dry mouth, constipation (from blocking muscarinic receptors) -hypotension (from blocking alpha-1 receptors -sedation (from blocking histamine receptors)
Neuroleptic malignant syndrome
toxicity of antipsychotics causing rigidity, myoglobinuria, autonomic instability and hyperpyrexia
Treatment forNeuroleptic malignant syndrome
-dantrolene -D2 agnoists (bromocriptine)
toxicity of antipsychotics casuing oral-facial movements
High potency antipsychotics
-Trifluoperazine, Fluphenazine, Haloperidol *these cause neurologic side effects (EPS system)
Low potency antipsychotics
-Chlorpromazine, Thioridazine *these cause non-neurologic side effects
Chlorpromazine can also cause…
Thioridazine can cause…
Haloperidol can also cause…
NMS or tardive dyskinesia.
Evolution of EPS side effects
-4 hr acute dystonia -4 day akathisia -4 wk bradykinesia -4 month tardive dyskinesia
Atypical Antipsychotics (6)
- Olanzpaine 2. Clozapine 3. Quetiapine 4. Risperidone 5. Aripiprazole 6. Ziprasidone
Clinical use of atypical antipsychotics
-schizophrenia (+ and - symptoms) -Bipolar -OCD -anxiety disorder -depression -mania -tourette’s
Olanzapine/Clozapine may cause…
significant weight gain.
Clozapine may cause…
agranulocytosis (requires weekly WBC monitoring) and seizure.
Risperidone may increase…
prolactin (lactation/gynecomastia) leading to decreased GnRH, LH and FSH (irregular menstruation/fertility).
prolong the QT interval.
Clinical use of Lithium
-mood stabilizer for bipolar disorder -blocks relapse and acute manic episodes -SIADH
Toxicity of Lithium
-tremor -sedation -edema -heart block -polyuria -teratogenesis
Lithium causes polyuria because…
it is an ADH antagonist causing nephrogenic DI.
Fetal cardiac defects from lithium include…
Ebstein anomaly and malformation of the great vessels.
stimulates 5-HT(1A) receptors
Use of Buspirone
-generalized anxiety disorder (1-2 wks to take effect) (does not interact with alcohol)
- Fluoxetine 2. Paroxetine 3. Sertraline 4. Citalopram
Mechanism of SSRIs
5-HT specific reuptake inhibitors
Use of SSRIs
-depression -GAD -Panic disorder -OCD -bulimia -social phobias -PTSD
Toxicity of SSRIs
-GI distress -sexual dysfunction -serotonin syndrome w/ any drug that increases 5HT (MAO inhibitors, SNRIs, TCAs)
-hyperthermia -confusion -myoclonus -CV collapse -flushing -diarrhea -seizures
Serotonin Syndrome is treated with…
Cyproheptadine (5-HT2 receptor antagonist)
For SSRIs to start taking effect, it takes…
Mechanism of SNRIs
inhibit 5-HT and NE reuptake
Use of SNRIs
depression -Venlafaxine also for GAD and panic disorder -Duloxetine also for diabetic peripheral neuropathy
Toxicity of SNRIs
increased BP stimulant effects sedation nausea
Tricyclic Antidepressants (7)
- amitriptyline 2. nortriptyline 3. imipramine 4. desipramine 5. clomipramine 6. doxepin 7. amoxapine
block reuptake of NE and 5-HT
Uses of TCAs
-depression -OCD (clomipramine) -fibromyalgia
Toxicity of TCAs
-sedation -alpha-1 blocking effects (postural hypotension) -atropine-like effects (anticholinergic - tachycardia, urinary retention, dry mouth) -convulsions -coma -cardiotoxicity -respiratory depression -hyperpyrexia
Tertiary TCAs (amitriptyline) have more…
anticholinergic effects than secondary TCAs (nortriptyline) have.
Desipramine is less…
sedating but has higher seizure incidence.
In the elderly, TCAs can cause…
confusion and hallucinations due to anticholinergic side effects (use nortriptyline).
Treatment for cardiotoxicity from TCAs
Monoamine oxidase inhibitors (4)
- Tranylcypromine 2. Phenelzine 3. Isocarboxazid 4. Selegine (slective MAO-B inhibitor)
Mechanism of MAO inhibitors
inhibition of MAO leading to increased levels of amine neurotransmitters (NE, 5-HT, DA)
use of MAO inhibitors
-atypical depression -anxiety -hypochondria
Toxicity of MAOIs
-hypertensive crisis (typically w/ ingestion of tyramine) -CNS stimulation
MAOIs are contraindicated with…
SSRIs TCAs St. John’s wort Meperidine Dextromethorphan
- Buproprion 2. Mirtazapine 3. Trazodone
NE and DA
Besides depression, buproprion is also used for…
Toxicity of Buproprion
-stimulant effects -HA -seizure in bulimic pts
-alpha2-antagonist (increased release of NE and 5-HT) -potent 5-HT2 and 5-HT3 antagonist
Toxicity of Mirtazapine
-sedation -increased appetite -weight gain -dry mouth
-blocks 5-HT2 and alpha1-adrenergic receptors
Trazodone is primarily used for…
Toxicity of Trazodone
sedation nausea priapism postural hypotension