Pharmacology: Psych/Neuro Flashcards
Methyphenidate
CNS stimulant
- Increase catecholamines in the synaptic cleft
Dextroamphetamine
CNS stimulant
- Increase catecholamines in the synaptic cleft
Mixed amphetamine salts
CNS stimulant
- Increase catecholamines in the synaptic cleft
Haloperidol
High potency, first generation antipsychotic
- Block DA2 receptors, incr cAMP
- Increased EPS: restlessness, involuntary mvmts, uncontrollable speech
Trifluoperazine
High potency, first generation antipsychotic
- Block DA2 receptors, incr cAMP
- Increased EPS: restlessness, involuntary mvmts, uncontrollable speech
Fluphenazine
High potency, first generation antipsychotic
- Block DA2 receptors, incr cAMP
- Increased EPS: restlessness, involuntary mvmts, uncontrollable speech
Chlorpromazine
Low potency, first generation antipsychotic
- Less EPS SEs
- More antiACh, antiH, anti-alpha SEs: dry mouth, sedating, hypotension
- CORNEAL deposits!
Thioridazine
Low potency, first generation antipsychotic
- Less EPS SEs
- More antiACh, antiH, anti-alpha SEs: dry mouth, sedating, hypotension
- reTinal deposits!
Eye effects of chlorpormazine vs. thioridazine
C: Corneal deposits
T: reTinal deposits (e.g. retinitis pigmentosa)
Dantrolene
Muscle relaxant
- Abolishes excitation-contraction coupling in muscle cells, probably by action on RyR
Tx: NMS (for muscle rigidity), malignant hyperthermia
Bromocriptine
D2 agonist
Tx: NMS
Order these EPS side effects in order of appearance: Akathisia Akinesia Acute dystonia Tardive dyskinesia
- Acute dystonia - 4 hrs
- Akinesia (parkinsonian sx) - 4 days
- Akathisia (restlessness/out of body feeling) - 4 wks
- Tardive dyskinesia (involuntary repetitive body movements) - 4 mos
Olanzapine
Atypical antipsychotic
- Various 5HT2, DA, alpha, H1 effects
Tx: Schizophrenia; Olanz also for OCD, anxiety, depression, mania, Tourette’s
SE: weight gain! (like clozapine)
Clozapine
Atypical antipsychotic
- Various 5HT2, DA, alpha, H1 effects
Tx: Schizophrenia
SE: weight gain (like olanzapine), seizures! agranulocytosis!
Quetiapine
Atypical antipsychotic
- Various 5HT2, DA, alpha, H1 effects
Tx: Schizophrenia
Risperidone
Atypical antipsychotic
- Various 5HT2, DA, alpha, H1 effects
Tx: Schizophrenia
Aripiprazole
Atypical antipsychotic
- Various 5HT2, DA, alpha, H1 effects
Tx: Schizophrenia
Ziprasidone
Atypical antipsychotic
- Various 5HT2, DA, alpha, H1 effects
Tx: Schizophrenia
SE: Prolong QT!
Which drugs have these SEs?
- Restlessness, involuntary mvmts, incontrollable speech
- Dry mouth, constipation, sedation, hypotension
- Weight gain
- Agranulocytosis
- Prolonged QT
- Typical, high potency antipsychs: haloperidol, trifluoperazine, fluphenazine
- Typical, low potency antipsychs: chlorpromazine (corneal), thioridazine (retinal)
- clozapine, olanzapine
- clozapine
- ziprasidone
Lithium
Mood stabilizer
- Unk MOA
Tx: BPD (blocks relapse and acute manic events), SIADH
SEs: MNOP
- Movement (tremor)
- Nephrogenic DI (ADH antagonist) resulting in polyuria
- hypOthyroid
- Pregnancy problems: Ebstein’s anomaly, malformation of the great vessels
Buspirone
Serotonin agonist
- Stimulates 5-HT1A receptors
- No sedation, addiction, tolerance
- No interaction with EtOH (unlike BZDs, barbs)
Amitriptyline
Tertiary TCA
- Blocks 5HT > NE reuptake
Tx: MDD, fibromyalgia
SE: more antiACh than secondary TCAs (tachycardia–M2 decr HR, urinary retention, more confusion and hallucinations in elderly –like AD), sedation
Toxicity: Convulsions! Coma! Cardiotoxicity! Resp depression, hyperpyrexia
Imipramine
Tertiary TCA - Blocks 5HT > NE reuptake Tx: MDD, fibromyalgia, BEDWETTING SE: antiACh effects, sedation Toxicity: Convulsions! Coma! Cardiotoxicity! Resp depression, hyperpyrexia
Clompramine
Tertiary TCA - Blocks 5HT > NE reuptake Tx: MDD, fibromyalgia, OCD SE: antiACh effects, sedation Toxicity: Convulsions! Coma! Cardiotoxicity! Resp depression, hyperpyrexia
Doxepin
Tertiary TCA - Blocks 5HT > NE reuptake Tx: MDD, fibromyalgia SE: antiACh effects, sedation Toxicity: Convulsions! Coma! Cardiotoxicity! Resp depression, hyperpyrexia
Tertiary vs. Secondary TCAs
Tertiary: 5HT > NE, more antiACh effects
- urinary retention, tachy, dry mouth
- confusion and hallucination in elderly
Secondary: NE > 5HT
Nortriptyline
Secondary TCA
- Blocks NE > 5HT reuptake
Tx: MDD, fibromyalgia
Better for elderly! Less anti-Ach effects (confusion, hallucinations)
Desipramine
Secondary TCA
- Blocks NE > 5HT reuptake
Tx: MDD, fibromyalgia
LEAST sedating! But lower sz threshold
Amoxapine
Secondary TCA
- Blocks NE > 5HT reuptake
Tx: MDD, fibromyalgia
NaHCO3
antidote for TCA toxicity
Fluoxetine
SSRI
Paroxetine
SSRI
Sertraline
SSRI
Citalopram
SSRI
Cyproheptadine
5-HT2 receptor antagonist
- treats Serotonin Syndrome (hyperthermia, myoclonus, CV collapse, flushing, diarrhea, seizures)
Venlafaxine
SNRI
Depression, GAD
Duloxetine
SNRI
Depression, diabetic peripheral neuropathy
Great effect on NE than venlafaxine
Tranylcypromine
MAOI
- incr NE. 5HT, DA
Atypical depression (hypersomnia, overeating, mood reactivity, weight gain, sensitivity to rejection); anxiety, hypochondriasis
SEs: Hypertensive crisis with Tyr ingestion and beta agonists; CNS stimulation
**Don’t give with SSRIs or meperidine (opioid) to prevent serotonin syndrome!!
Phenelzine
MAOI
- incr NE. 5HT, DA
Atypical depression; anxiety; hypochondriasis
SEs: Hypertensive crisis with Tyr ingestion and beta agonists; CNS stimulation
**Don’t give with SSRIs or meperidine (opioid) to prevent serotonin syndrome!!
Isocarboxazid
MAOI
- incr NE. 5HT, DA
Tx: Atypical depression; anxiety; hypochondriasis
SEs: Hypertensive crisis with Tyr ingestion and beta agonists; CNS stimulation
**Don’t give with SSRIs or meperidine (opioid) to prevent serotonin syndrome!!
Selegiline
MAO-I (MAOB selective, which is more location specific - neurons, astroglia, plts)
- incr NE. 5HT, DA
Tx: Parkinson’s; atypical depression; anxiety; hypochondriasis
SEs: Hypertensive crisis with Tyr ingestion and beta agonists; CNS stimulation
**Don’t give with SSRIs or meperidine (opioid) to prevent serotonin syndrome!!
Buproprion
Atypical antidepressant - Incr NE and DA (unk MOA) Tx: depression, smoking cessation **Sz in bulimic pts! No sexual SE
Mirtazapine
Atypical antidepressant
- alpha2 antagonist, incr release of NE and 5HT via decr neg feedback
- potent 5HT2 and 5HT3 antagonist
SE: incr appetite! sedation, weight gain, dry mouth
Maprotiline
Atypical antidepressant
- Blocks NE reuptake
SE: sedation, orthostatic hypotension
Trazodone
Atypical antidepressant
- Main action is to inhibit 5HT reuptake
Tx: insomnia
SEs: PRIAPISM, postural hypotension, sedation, nausea
Epinephrine
Alpha-agonist
- Decrease aqueous humor due to vasconstriction
SE: mydrasis (do not use in closed-angle glaucoma!); stinging
Brimondine
Alpha-agonist
- Decrease aqueous humor due to vasconstriction
SE: no pupillary or vision changes
Timolol
Beta-blocker
- Decrease aqueous humor due to vasconstriction
SE: no pupillary or vision changes
Betaxolol
Beta-blocker
- Decrease aqueous humor due to vasconstriction
SE: no pupillary or vision changes
Carteolol
Beta-blocker
- Decrease aqueous humor due to vasconstriction
SE: no pupillary or vision changes
Acetazolamide
Diuretic, inh CA
- Decrease aqueous humor due to decr HCO3-
SE: no pupillary or vision changes
Pilocarpine
Direct cholinomimetic
- incr aqueous humor outflow, contract ciliary muscle and open trabecular meshwork
SE: miosis, cyclospasm (contraction of the ciliary muscle in the eye)
**Pilocarpine good for emergencies! Good for opening meshwork into canal of Schlemm
Carbachol
Direct cholinomimetic
- incr aqueous humor outflow, contract ciliary muscle and open trabecular meshwork
SE: miosis, cyclospasm (contraction of the ciliary muscle in the eye)
Physostigmine
Indirect cholinomimetic
- incr aqueous humor outflow, contract ciliary muscle and open trabecular meshwork
SE: miosis, cyclospasm (contraction of the ciliary muscle in the eye)
Echothiopate
Indirect cholinomimetic
- incr aqueous humor outflow, contract ciliary muscle and open trabecular meshwork
SE: miosis, cyclospasm (contraction of the ciliary muscle in the eye)
Latanoprost
Prostaglandin (PGF2alpha)
- Increase outflow of aqueous humor
SE: darkens iris (browning)
Morphine
Opioid analgesic
Fentanyl
Opioid analgesic
Codeine
Opioid analgesic
Heroin
Opioid analgesic
Methadone
Opioid analgesic
Detromethorphan
Opioid analgesic
- Cough suppr
Deiphenoxylate
Opioid analgesic
- For diarrhea
Loperamide
Opioid analgesic
- For diarrhea
Opioid tolerance does NOT develop to…
- miosis
2. constipation
Butorphanol
Partial agonist at mu opiod receptors, agonist at kappa receptors
- Causes w/d if on full opioid agonist
Tramadol
Very weak opioid agonist, also inhibits 5HT and NE
- Decreases sz threshold
Phenytoin
Na channel inactivation
1st line: GTC, Status PPX (vs BZD for acute)
Also: Simple- and complex-partial
Fosphenytoin (IV form)
Na channel inactivation
1st line: GTC, Status
Also: Simple- and complex-partial
Carbamazepine
Na channel inactivation
1st line: Trigeminal neuralgia, GTC, simple- and complex-partial
Lamotrigine
Na channel inactivation
Gabapentin
GABA analog, but inhibits Ca2+ channels
Peripheral neuropathy, BPD
VPA
Na channel inactivation, incr GABA
1st line: GTCs, myoclonic seizures
Topiramate
Na channel inactivation, incr GABA
Phenobarbital
Barbiturate, incr GABA via incr DURATION of Cl- channel opening (vs. BZD incr freq)
1st line: pregnant women and children
- incr P450
Ethosuximde
Blocks T type Ca channels
1st line: Absence
SJS
Diazepam
Lond acting BZD, incr GABA action by incr FREQ of Cl- channel opening
1st line: acute status
Lorazepam
Intermediate BZD, incr GABA action by incr FREQ of Cl- channel opening
1st line: acute status
Tigabine
Inh GABA reuptake
Vigabatrin
Incr GABA via irrev inhibition of GABA transaminase
Levetriacetam
Unk MOA, may modulate GABA and Glu release
Pentobarbital
Barbiturate, incr GABA via incr DURATION of Cl- channel opening (vs. BZD incr freq)
1st line: pregnant women and children
- incr P450
Thiopental
Barbiturate, incr GABA via incr DURATION of Cl- channel opening (vs. BZD incr freq)
- 1st line: pregnant women and children
- Anesthesia induction (high lipid solubility, high potency)
- incr P450
- DECR cerebral BF (may incr cerebral metabolic demand?)
Secobarbital
Barbiturate, incr GABA via incr DURATION of Cl- channel opening (vs. BZD incr freq)
1st line: pregnant women and children
- incr P450
Triazolam
Short acting BZD
Alprazolam
Short acting BZD
Oxazepam
Short acting BZD
Midazolam
Short acting BZD
Estrazolam
Intermediate acting BZD (along with lorazepam and temazepam)
Temazepam
Intermediate acting BZD (along with lorazepam and estrazolam)
Flurazepam
Long acting BZD (along with diazepam, chlordiazepoxide, clorazepate)
Chlordiazepoxide
Long acting BZD (along with diazepam, flurazepam, clorazepate)
Clorazepate
Long acting BZD (along with diazepam, chlordiazepoxide, flurazepam)
Zolpedim
aka Ambien
Non-BZD hypnotic
Zaleplon
Non-BZD hypnotic
Eszopiclone
Non-BZD hypnotic
Flumazenil
Competitive antagonist at GABA BZD receptor site
- OD of BZD or non-BZD hypnotics
Halothane
Inhaled anesthetic
- Hepatotoxicity
Enflurane
Inhaled anesthetic
- Proconvulsant
Isoflurane
Inhaled anesthetic
Sevoflurane
Inhaled anesthetic
Methoxyflurane
Inhaled anesthetic
- Nephrotoxicity
NO
Inhaled anesthetic
SE: expansion of trapped gas
Arylcyclohexylamines (Ketamine)
Dissociative anesthetic
- Blocks NMDA receptor
- Incr cerebral BF (decr cerebral metabolic demand)
SE: CV stimulation
Propofol
Potentiates GABA
- Rapid anesthesia induction and short procedures
Procaine
Ester local anesthetic
- block Na ch
Cocaine
Ester local anesthetic
- block Na ch
SE: HTN, hypotension, arrhythmia
Tetracaine
Ester local anesthetic
- block Na ch
Lidocaine
Amide local anesthetic (give if ester allergic)
- block Na ch
Mepivacaine
Amide local anesthetic (give if ester allergic)
- block Na ch
Bupivacaine
Amide local anesthetic (give if ester allergic)
- block Na ch
SE: Severe CV tox!
Succinylcholine
Depolarizing NM blocking agent
- Phase I (prolonged depol): no antidote, potentiated by AChE-I
- Phase II (repol but not blocked): give AChE-I e.g. neostigmine as antidote
Tubocurarine
Non-depolarizing NM blocking agent
- Competitive ACh R antagonist
Rev blockade with AChE-I (neostigmine, edrophonium)
Atracurium
Non-depolarizing NM blocking agent
- Competitive ACh R antagonist
Rev blockade with AChE-I (neostigmine, edrophonium)
Mivacurium
Non-depolarizing NM blocking agent
- Competitive ACh R antagonist
Rev blockade with AChE-I (neostigmine, edrophonium)
Pancuronium
Non-depolarizing NM blocking agent
- Competitive ACh R antagonist
Rev blockade with AChE-I (neostigmine, edrophonium)
Vecuronium
Non-depolarizing NM blocking agent
- Competitive ACh R antagonist
Rev blockade with AChE-I (neostigmine, edrophonium)
Rocuronium
Non-depolarizing NM blocking agent
- Competitive ACh R antagonist
Rev blockade with AChE-I (neostigmine, edrophonium)
Dantrolene
Prevents release of Ca from SR of skeletal muscle
- Malignant hyperthermia
- NMS
Bromocriptine
DA agonist
ergot (not preferred)
Pramipexole
DA agonist
Ropinirole
DA agonist
non-ergot (preferred)
Amantadine
Incr DA release, blocks viral uncoating (M2 protein)
L-dopa/carbidopa
Incr DA in CNS
- Carbidopa inh periph decarboxylase
SE: ARRHYTHMIAS from peripheral conversion of DA
Selegiline
selective MAOB inh (MAOB prefers to metabolize DA)
- Prevent L-dopa degradation
Entacapone
COMT inh
- Prevent L-dopa degradation
Tolcapone
COMT inh
- Prevent L-dopa degradation
Benztropine
Antimuscarinic, improves tremor and rigidity but little effect on bradykinesia
Baclofen
GABA derivative, GABA-B agonist
For spasticity and alcoholism
Memantine
NMDA R antagonist
- prevent excitotoxicity mediated by Ca
Alzheimers
Donepezil
AchE inhibitor
Alzheimers
Galantamine
AchE inhibitor
Alzheimers
Rivastigmine
AchE inhibitor
Alzheimers
Vit E
Antioxidant
Reserpine
blocks the vesicular monoamine transporter (VMAT), prevent NT packaging into vesicles and release (they then get degraded by MAO and COMT)
- Huntington’s (hyperkinetic mvmnt)
Tetrabenazine
blocks the vesicular monoamine transporter (VMAT), prevent NT packaging into vesicles and release (they then get degraded by MAO and COMT)
- Huntington’s (hyperkinetic mvmnt)
Sumatriptan
5-HT1B/1D agonist
- Vasocontriction, inh trigeminal activation and Vasoactive peptide relsease
Tx: acute migraine, cluster Ha
SE: coronary vasospasm!
