Professional Documents
Culture Documents
1
Antidepressants
General comments:
- All drugs involve phosphorylation in their mechanism of action (resulting in changes in release, cytoskeleton, gene expression) thus
clinical improvement may take several weeks
- All drugs have immediate pharmacological actions
Class
blockade)
Reversal of methyldopa, clonidine
activity
Adverse
Sexual
Weight loss
Seizures (fluoxetine only) due
to seizure threshold
- Fluoxetine 76 hrs; sertraline 23 hrs
Acute toxicity: < than TCAs
or MAOIs
Uses:
Drug Interactions:
- Depression
MAOIs: Serotonin syndrome tremor, hyperthermia,
- Obsessive-compulsive disorder (OCD)
CV collapse.
(Obviously) life-threatening
MAOI use before starting SSRIs
- Bulemia
Fluoxetine inhibits cytP-450 (CYP2D6)
- Not used for enuresis or pain
Inhibits dopamine and norepinephrine
Duration: t = 11-14 hrs
Atypical
Bupropion
Adverse effects:
antidepressants
(Welbutrin, Zyban)
reuptake (better at blocking dopamine)
Reduces nicotine craving
toxicities (not antimuscarinic)
Not antimuscarinic or sedating
Seizures
NO hypotension/cardiac
Drug Interactions:
Nefazodone
Blocks serotonin reuptake (5HT2A and
mild orthostatic hypotension, impotence
5HT2C receptors)
Mirtazapine
2-adrenergic antagonist
Duration: t= 20-40 hrs
mild orthostatic hypotension
Carbamazepine metabolism
Adverse effects: sedation,
Adverse
Adverse
Tyramine
pickled herring, sardines)
headache,
Orthostatic
Atropine-like
Tremors, insomnia,
Hepatotoxicity
Drug Interactions:
Elevate mood
diarrhea
Excretion: Renal
Nausea, vomiting,
Pharmacokinetics of alcohol
Absorption/Distribution: Lipid soluble; absorbed through oral/GI mucosa and widely distributed
Metabolism
Excretion
Withdrawal
Narrow therapeutic
window
(phosphodiesterase, PDE, at higher doses) Distribution: Tissues, crosses placenta
CNS:
Seizures, insomnia, motor impairment, tremors
Metabolism: Liver
Cardiac arrhythmias
Theobromine
Amphetamines
Dextramphetamine
Mechanism: DA in synaptic cleft Admin/Absorption: Oral; well-absorbed in GI
Pemoline (Cylert )
Competitively inhibits DA/NE transp. Metabolism: Liver
Insomnia
2+
Ca -independent release of NE Excretion: Renal
GI upset
Competitive inhibition of MAO Duration of action: t (Ritalin) < t (Cylert)
Headaches
Uses: Ritalin/Cylert: ADHD
Drug interactions: MAO
inhibitors, drugs affecting DA/NE
Cocaine
Action: Blocks Na+-activated ATPase, and
Potentiates
adrenergic agonists
thus reuptake of NE into the adrenergic
Tonic-clonic seizures (high
doses)
nerve terminal; NE stays around longer,
Cardiac arrhythmias
causing sympathetic stimulation
Respiratory depression (high
doses)
Effects:
conjugate to form
Anorexiants
pressure
Sibutramine
Increased blood
Clinical Uses
Schizophrenia
Tourettes syndrome (tics, curses)
Acute psychotic disorders
Anesthetic adjunct
Drug (amphetamine, LSD)-induced psychoses
Antiemetic
of choice!)
Antipruritic
Intractable hiccups
Initial Rx for bipolar disorder (remember, lithium is drug
Pharmacokinetics
Absorption/Distribution: Lipid soluble; well-absorbed in GI tract. Distributes to CNS; large volume of distribution
Metabolism: Extensive 1st pass metabolism, to active metabolites!
Class
Haloperidol (Haldol )
High D2 blockade
Extrapyramidal side-effects (> than chlorpromazine)
Low 1, H1, M1 blockade
- Dystonias spastic reactions (1 week)
- Akathesias (restlessness) (3 weeks)
- Parkinson-like symptoms (tremors, rigidity, etc).(1-2 months)
- Tardive dyskinesia (irreversible!) (12-16 months)
Neuroleptic malignant syndrome: severe musuclar rigidity, body temp,
impaired sweating. Seen more in patients
experiencing Parkinsons symptoms.
DA prolactin gynecomastia, infertility, galactorrhea-amenorrhea
syndrome
1-receptor blockade: postural hypotension, impotence, failure to ejaculate (<
than chlorpromazine)
Muscarinic receptor blockade: dry mouth, constipation, urinary retention,
visual problems (< than chlorpromazine)
Risperidone (Risperidal )
Very low D2 blockade
Extrapyramidal side-effects: < than typicals
Low 1, H1, M1 blockade
1, histaminic, muscarinic blockade low to moderate side-effects
5-HT2 blockade
Mechs of Action/Effects
Drug-specific Uses
Pharmacokinetics
Adverse Effects
Atropine
High levels
hypotension, CV effects
Effects as disease
Carbidopa
Tolcapone
toxicity
(Eldepryl ) Neuroprotective!!
use of dopa (neuroprotective)
Amantadine synthesis, release, re-uptake of DA
Also an antiviral drug
agitation; psychosis with high doses
Liver
Bromocriptine: D1-related
Ergot alkaloids:
All dopamine agonists:
Restlesslessness,
Orthostatic hypotension, urinary retention,
dry mouth
Baclofen
Mechanism of action/Effects
Uses
Adverse Effects
Benzodiazepines
Binds to benzodiazepine receptor adjacent Chlordiazepoxide (Librium) Long-acting Anti-anxiety (but not OCD)
Sedation
to the GABAA receptor, increasing the
Insomnia
Insomnia
Flurazepam (Dalmane)
Long-acting
Alprazolam (Xanax)
Temazepam (Restoril)
Lorazepam (Ativan)
Intermediate-acting
Insomnia
Triazolam (Halcion)
Very short-acting
Insomnia
(behavioral problems)
Bizarre behavior
asleep afterwards)
Anterograde amnesia (blocks process of
recent learning)
Oxazepam
Midazolam
Short-acting
Short-acting
Insomnia
Insomnia
Date-rape drug formulation
Mechanism of action/Effects
Barbiturates
Uses
Insomnia
Mechs of Action/Effects
Uses
Pharmacokinetics
Adverse Effects
Phenytoin
Inhibits voltage-gated Na+ channel Focal seizures
Admin/Absorption: Oral, variable absorption
CNS:
Nystagmus, diplopia, ataxia, sedation/seizures (high dose)
Tonic-clonic seizures
Distribution: > 90% protein-bound (displaceable) GI: Nausea,
vomiting
Metabolism: Not first order, but hydroxylated to Endocrine: Increased
metabolism of Vitamin D, interference of
inactive metabolite
Ca2+ absorption (can lead to
osteomalacia)
Altered tissue growth: Hirsutism,
thickened facial features,
gingival hyperplasia
Megaloblastic anemia (due to increase of
folate metabolism)
Carbamazepine
Inhibits voltage-gated Na+ channel Focal seizures
Diplopia, ataxia, sedation (less serious than phenytoin)
(rare)
Ethosuximide Inhibits T-type Ca2+ channel
at high doses
Absence seizures
(drug of choice)
pain
Hiccups
Metabolism: Hydroxylation (metabolite is active)
Diazepam
Clonazepam
develop
CNS:
Teratogenic
Affects clearance of phenytoin,
Narrow therapeutic
Sedation, ataxia
Inducer of CYP450
Contraindicated with porphyrias
Tolerance can
Narrow therapeutic window
Felbamate
Hepatotoxicity
Aplastic
anemia
(Lenox-Gestalt Syndrome)
Pharmacology Review Sheets: Neuro Drugs, p.7
Antihistamines
Type
Drugs
Duration
Uses
Sedation
Antihistamines
H1 receptor
Antitussive
Antimuscarinic effects: dry mouth,
blurry vision, constipation
(H1 blockade)
Muscarinic cholinergic blockade
OTC sleep aid
Convulsions (esp. in
kids)
-adrenergic blockade
Dimenhydrinate (Dramamine)
Anti-motion sickness
Excitation
(elderly) Sundown condition
5-HT receptor blockade
Meclizine (Antivert)
Long (12-24 h)
Anti-motion sickness
Postural
hypotension (-blockade)
Local anesthetic
Chlorpheniramine
OTC cold remedy
Drug allergy
(topical use)
(ChlorTrimeton)
Promethazine (Phenergan)
Anti-emetic
nd
2 generation More selective H1-receptor blockade
Citeridine (Zyrtec)
Allergic rhinitis/urticaria Minimal
sedation
Antihistamines
No anesthetic effects
Loratidine (Claritin)
Allergic rhinitis/urticaria No
anticholinergic effects
(H1 blockade)
Longer acting
Fexofenadine (Allegra)
Allergic rhinitis/urticaria No
antisertoninergic effects
CV: QT prolongaion, arrhythmias
H2 - specific Block gastric acid secretion by blocking Cimetidine (Tagamet)
Peptic duodenal, gastric ulcers
CNS:
delirium, confusion (elderly); dizziness, headache
Ranitidine (Zantac)
Zollinger-Ellison syndrome,
Anti-
Erosive esophagitis
Blood dyscrasias
Inhibits CYP-450
GI: Hepatotoxicity, diarrhea
Skin: Rash
Peptic duodenal, gastric ulcers
CNS: Diziness,
headache
Zollinger-Ellison syndrome GI: Hepatotoxicity, diarrhea
Erosive esophagitis
Skin: rash
Famotidine (Pepcid)
headache
CNS: Diziness,
CNS: Diziness,
headache
Zollinger-Ellison syndrome GI: Hepatotoxicity, diarrhea
Erosive esophagitis
Skin: rash