Final Review Blocks 1-3 Flashcards
Norepinephrine
Mixed Agonist (Adrenergic)
- A1, A2, and B1
Epinephrine
Mixed Agonist (Adrenergic)
- A1, A2, B1, B2
- low doses = B1 and B2, high doses = A1
- treat acute anaphylaxis or cardiac arrest
Cocaine
NET, DAT, SERT Inhibitor (Adrenergic)
- vasoconstriction, MI, stroke, death
Methylphenidate
NET, DAT Inhibitor (Adrenergic)
- ADHD and narcolepsy tx
- anorexia, jitters, poor growth, priapism
Atomoxetine
NET Inhibitor (Adrenergic)
- ADHD tx
- low abuse potential because non-stimulant
Ephedrine / Pseudoephedrine
Indirect Sympathomimetic (Adrenergic)
- increase BP and HR
- don’t use with MAOi
Amphetamine / Methamphetamine
Indirect Sympathomimetic (Adrenergic)
- 1st line for ADHD in low doses
- jitters, poor growth, anorexia, addictive
Phenylephrine
A1 Agonist (Adrenergic)
- vasoconstriction
- used for decongestant, hemorrhoids, mydriasis
Clonidine
A2 Agonist (Adrenergic)
- treat HTN, ADHD, neuropathic pain
- causes hypotension, sedation, dry mouth
Phenoxybenzamine
Nonselective Alpha Antagonist (Adrenergic)
- non-competitive and irreversible
- A1 and A2 antagonist
- pheochromocytoma tx
Phentolamine
Nonselective Alpha Antagonist (Adrenergic)
- competitive and reversible
- A1 and A2 antagonist
- pheochromocytoma tx
Prazosin
A1 Antagonist (Adrenergic)
- decreases peripheral vascular resistance
- treats HTN, BPH, Raynaud’s
- “first dose phenomenon” = hypotension and syncope with first dose
Tamsulosin
A1 Antagonist (Adrenergic)
- decreases peripheral vascular resistance, more selective for prostatic urethra
- treats BPH primarily
- “first dose phenomenon” = hypotension and syncope with first dose
Dobutamine
B1 Agonist (Adrenergic)
- cardiac stimulation and renin release
- used for cardiac failure
- dysrhythmias
Albuterol
B2 Agonist (Adrenergic)
- Short acting
- Asthma and COPD tx
Terbutaline
B2 Agonist (Adrenergic)
- Short acting
- Asthma and COPD tx
Salmeterol
B2 Agonist (Adrenergic)
- long acting
- persistent asthma and COPD
Mirabegron
B3 Agonist (Adrenergic)
- OAB tx
- slow onset, can cause HTN
Esmolol
B1 Selective Antagonist (Adrenergic)
- tx for HTN, angina, arrhythmia, ischemia
- also used for intraoperative HTN
- rebound HTN = taper dose
- bronchoconstriction, bradycardia, CNS effects
- short half life
Metoprolol
B1 Selective Antagonist (Adrenergic)
- tx for HTN, angina, arrhythmia, ischemia
- also used for intraoperative HTN
- rebound HTN = taper dose
- bronchoconstriction, bradycardia, CNS effects
Propanolol
B1/B2 Nonselective Antagonist (Adrenergic)
- tx for HTN, angina, arrhythmia, ischemia
- migraine prophylaxis
- caution with asthma due to B2 effects
- rebound HTN = taper dose
- bronchoconstriction, bradycardia, CNS effects
Timolol
B1/B2 Nonselective Antagonist (Adrenergic)
- decreases aqueous humor production and reduces intraocular pressure
- bronchoconstriction, bradycardia, CNS effects
Labetalol
A/B Nonselective Antagonist (Adrenergic)
- Mostly B1 and B2 antagonism with some A1
- HTN tx and for Hypertensive Emergency
- rebound HTN = taper dose
- bronchoconstriction, bradycardia, CNS effects
Carvedilol
A/B Nonselective Antagonist (Adrenergic)
- 10:1 B1 and B2 to A1 antagonism
- HTN, HF
- rebound HTN = taper dose
- bronchoconstriction, bradycardia, CNS effects
Methacholine
Muscarinic Agonist (Cholinergic)
Pilocarpine
Muscarinic Agonist (Cholinergic)
- open angle glaucoma tx
- DUMBBELS
- sweating
Bethanecol
Muscarinic Agonist (Cholinergic)
- GI stimulation / inactive bowel
- urinary retention tx
- DUMBBELS and sweating
Atropine
Muscarinic Antagonist (Cholinergic)
- mydriasis tx
- antidote for muscarinic toxicity, can cross BBB
- DUMBBELS and sweating
Scopolamine
Muscarinic Antagonist (Cholinergic)
- motion sickness tx
Ipratropium
Muscarinic Antagonist (Cholinergic)
- asthma and COPD tx
Glycopyrrolate
Muscarinic Antagonist (Cholinergic)
- used prep to decrease secretions and gastric acidity
Darifenacin
Muscarinic Antagonist (Cholinergic)
- M3 selective antagonist
- treats OAB
Benztropine
Muscarinic Antagonist (Cholinergic)
- PSNS symptoms, including confusion
- AVOID IN ELDERLY AND COGNITIVELY IMPAIRED
- can treat Parkinson’s and extrapyramidal symptoms
Nicotine
Nicotinic Agent (Cholinergic)
- used for smoking cessation
- can develop tolerance or dependence
Varenicline
Nicotinic Agent (Cholinergic)
- partial agonist for smoking cessation
- can cause depression and suicidal ideation
Rocuronium
Nicotinic NMJ Antagonist (Cholinergic)
- skeletal muscle relaxer, useful in intubation
- prolonged paralysis can occur
Succinylcholine
Depolarizing NMJ Blockade (Cholinergic)
- activates nicotinic receptor before blocking it
- skeletal muscle relaxation during anesthesia, useful for intubation
- muscle soreness (potential hyperkalemia), malignant hypothermia
Donepezil
Acetylcholinesterase Inhibitor (Cholinergic)
- used for Alzheimer’s, improves cognition
Pyridostigmine
Acetylcholinesterase Inhibitor (Cholinergic)
- reversible carbamate substrate
- does NOT cross BBB
Neostigmine
Acetylcholinesterase Inhibitor (Cholinergic)
- reversible carbamate substrate
- does NOT cross BBB
- causes contraction of denervated skeletal muscle
Physostigmine
Acetylcholinesterase Inhibitor (Cholinergic)
- Readily crosses the BBB
- DUMBBELS side effects
- can treat atropine overdose
Edrophonium
Acetylcholinesterase Inhibitor (Cholinergic)
- reversible substrate
- very short acting, used for myasthenia gravis
Pralidoxome (2-PAM)
Acetylcholinesterase Poisoning Antidote (Cholinergic)
- does not cross BBB
- treats organophosphate toxicity, reverses NMJ blockade paralysis
Atropine
Acetylcholinesterase Poisoning Antidote (Cholinergic)
- Crosses BBB
- treats organophosphate toxicity, reverses NMJ blockade paralysis
Sarin
Toxic Organophosphate (Cholinergic)
- nerve gas
- DUMBBELS
Malathion
Toxic Organophosphate (Cholinergic)
- insecticide
- DUMBBELS
Amitriptyline
Tricyclic Antidepressant
- NET / SERT inhibitor
- also blocks muscarinic, A1, A2
- Causes coma, cardio toxicity, convulsions (3 Cs)
- sexual dysfunction, serotonin syndrome with MAOi
Nortriptyline
Tricyclic Antidepressant
- Primarily NET inhibitor
- also blocks muscarinic, A1, A2
- Causes coma, cardio toxicity, convulsions (3 Cs)
- sexual dysfunction, serotonin syndrome with MAOi
Imipramine
Tricyclic Antidepressant
- NET / SERT inhibitor
- also blocks muscarinic, A1, A2
- Causes coma, cardio toxicity, convulsions (3 Cs)
- sexual dysfunction, serotonin syndrome with MAOi
Sertraline
SSRI
- can cause GI issues, CNS issues, sexual dysfunction
- can precipitate mania in bipolar pt
- SSRI withdrawal: FLUSH
- risk of serotonin syndrome with MAOi
Citalopram
SSRI
- can cause GI issues, CNS issues, sexual dysfunction
- can precipitate mania in bipolar pt
- SSRI withdrawal: FLUSH
- risk of serotonin syndrome with MAOi
Fluoxetine
SSRI
- can cause GI issues, CNS issues, sexual dysfunction
- can precipitate mania in bipolar pt
- SSRI withdrawal: FLUSH
- risk of serotonin syndrome with MAOi
Paroxetine
SSRI
- can cause GI issues, CNS issues, sexual dysfunction
- can precipitate mania in bipolar pt
- SSRI withdrawal: FLUSH
- risk of serotonin syndrome with MAOi
Escitalopram
SSRI
- can cause GI issues, CNS issues, sexual dysfunction
- can precipitate mania in bipolar pt
- SSRI withdrawal: FLUSH
- risk of serotonin syndrome with MAOi
Venlafaxine
SNRI (Serotonin-Norepinephrine)
- dose dependent inhibition, same side effects as SSRI
- Low: SERT
- Mid: SERT/NET
- High: SERT/NET/DAT
Duloxetine
SNRI (Serotonin-Norepinephrine)
- selective NET/SERT inhibition, same side effects as SSRI
Bupropion
Atypical Antidepressant
- weak inhibition of NET/DAT/SERT
- nicotinic antagonist
- NO SEXUAL DYSFUNCTION
Mirtazapine
Atypical Antidepressant
- block A adrenergic and serotonin
- increased appetite and weight gain = GOOD FOR ELDERLY
- NO SEXUAL DYSFUNCTION
Trazodone
Serotonin Modulator
- weak SERT inhibition
- NO SEXUAL DYSFUNCTION
- off label treatment for insomnia
Vilazodone
Serotonin Modulator
- partial serotonin agonist
- insomnia side effect
- causes sexual dysfunction
St. John’s Wart
Herbal Supplement (Antidepressant)
- Hypericin –> MAO inhibitor
- Hyperforin –> NET/DAT/SERT inhibitor
Lithium
Mood Stabilizer (Bipolar / Antipsychotic)
- not safe in pregnancy
- needs regular renal and thyroid monitoring
Valproic Acid
Antiepileptic - Mood Stabilizer (Bipolar / Antipsychotic)
- prolongs Na channel inactivation and suppresses Ca influx
- increases GABA
- hepatotoxic
- contraindicated in pregnancy
Lamotrigine
Antiepileptic - Mood Stabilizer (Bipolar / Antipsychotic)
- inhibit glutamate release
- CAUSES STEVEN-JOHNSON RASH
- SAFE IN PREGNANCY
Haloperidol
High Potency Typical Antipsychotic (Bipolar / Antipsychotic)
- blocks D2 receptors
- frequent extrapyramidal effects, high risk of tardive dyskinesia
- prolongs QT interval
Chlorpromazine
Low Potency Typical Antipsychotic (Bipolar / Antipsychotic)
- also blocks muscarinic, histamine, A adrenergic receptors
- rare extrapyrimidal effects, low risk of tardive dyskinesia
Clozapine
Atypical Antipsychotic (Bipolar / Antipsychotic)
- 1st line class for schizophrenia
- block D2 and 5HT receptors
- rare extrapyramidal effects
Aripiprazole
Atypical Antipsychotic (Bipolar / Antipsychotic)
- 1st line class for schizophrenia
- block D2 and 5HT receptors
- rare extrapyramidal effects
- low incidence of weight gain
Olanzapine
Atypical Antipsychotic (Bipolar / Antipsychotic)
- 1st line class for schizophrenia
- block D2 and 5HT receptors
- rare extrapyramidal effects
- SIGNIFICANT WEIGHT GAIN and sedation
Ziprasidone
Atypical Antipsychotic (Bipolar / Antipsychotic)
- 1st line class for schizophrenia
- block D2 and 5HT receptors
- rare extrapyramidal effects
- PROLONGED QT INTERVAL
Quetiapine
Atypical Antipsychotic (Bipolar / Antipsychotic)
- 1st line class for schizophrenia
- block D2 and 5HT receptors
- rare extrapyramidal effects
- weight gain and tachycardia
- ABUSE POTENTIAL
Risperidone
Atypical Antipsychotic (Bipolar / Antipsychotic)
- 1st line class for schizophrenia
- block D2 and 5HT receptors
- HIGHER extrapyramidal risk
- PROLONGED QT INTERVAL
- INCREASED PROLACTIN AND GYNECOMASTIA IN MALES
Midazolam
Short Acting Benzodiazepine (Anxiolytic)
- positive allosteric modulator at GABAa
- respiratory depression, impaired memory and cognitive function
Triazolam
Short Acting Benzodiazepine (Anxiolytic)
- positive allosteric modulator at GABAa
- respiratory depression, impaired memory and cognitive function
Alprazolam
Intermediate Acting Benzodiazepine (Anxiolytic)
- positive allosteric modulator at GABAa
- respiratory depression, impaired memory and cognitive function
Lorazepam
Intermediate Acting Benzodiazepine (Anxiolytic)
- positive allosteric modulator at GABAa
- respiratory depression, impaired memory and cognitive function
Clonazepam
Long Acting Benzodiazepine (Anxiolytic)
- respiratory depression, impaired memory and cognitive function
Diazepam
Long Acting Benzodiazepine (Anxiolytic)
- respiratory depression, impaired memory and cognitive function
- treat alcohol withdrawal and bento withdrawal
Buspirone
Non-GABA Anxiolytic
- serotonin partial agonist, D2 antagonist
Flumazenil
Non-GABA Anxiolytic
- GABAa antagonist
- CAN INDUCE BENZO WITHDRAWAL OR SEIZURE
- USED FOR BENZO REVERSAL
Zolpidem
Z-Drug (Anxiolytic)
- GABAa agonist
- for insomnia
Zaleplon
Z-Drug (Anxiolytic)
- GABAa positive allosteric modulator
- for insomnia
- causes aggression and hallucination so NO IN ELEDERLY
Eszoplicone
Z-Drug (Anxiolytic)
- GABAa agonist
- for insomnia, CAN BE USED LONG TERM
Suvorexant
Sleep Drug (Anxiolytic)
- orexin antagonist
Doxepin
Sleep Drug (Anxiolytic)
- selective H1 antagonist at low doses, 5HT and D2 at higher doses
- don’t use with MAOi –> serotonin syndrome
Ramelteon
Sleep Drug (Anxiolytic)
- melatonin agonist
Trazodone
Sleep Drug / Atypical Antidepressant (Anxiolytic)
- increase serotonin, decrease histamine
Mirtazapine
Sleep Drug / Atypical Antidepressant (Anxiolytic)
- increase serotonin, decrease histamine
- good for elderly, hyperphagia and weight gain
Diphenhydramine
Sleep Drug / Atypical Antidepressant (Anxiolytic)
- increase serotonin, decrease histamine
- concern in elderly
Phenobarbital
Barbiturates (Anxiolytic)
- long acting GABAa agonist
- respiratory depression
- high concentration doesn’t require GABA binding
Pentobarbital
Barbiturates (Anxiolytic)
- short acting GABAa agonist
- respiratory depression
- high concentration doesn’t require GABA binding
Propofol
GABA Associated Anxiolytic
- GABAa agonist
- anesthetic
Baclofen
GABA Associated Anxiolytic
- ONLY GABAb agonist
Chloral Hydrate
GABA Associated Anxiolytic
- sedative, alleviates insomnia
- incapacitates individuals in prison
Phenytoin
Na+ Channel Anti-Epileptic
- arrhythmia
- teratogenic
Carbamazepine
Na+ Channel Anti-Epileptic
- bone marrow suppression
- neural tube defects in pregnancy
Lacosamide
Na+ Channel Anti-Epileptic
- well tolerated
Lamotrigine
Na+ Channel Anti-Epileptic
- epilepsy, bipolar, or depression
- inhibits glutamate as well
- CAUSES STEVENS-JOHNSON RASH
- SAFE IN PREGNANCY
Topiramate
Na+ Channel Anti-Epileptic
- CAUSES WEIGHT LOSS
- metabolic acidosis and cleft palate (teratogenic)
Ethosuximide
Ca2+ Channel Inhibitor Anti-Epileptic
- very safe and effective
Valproic Acid
Ca2+ Channel Inhibitor Anti-Epileptic
- hair loss, bruising, liver injury
- TERATOGENIC - SPINA BIFIDA
Gabapentin
Ca2+ Channel Anti-Epileptic
- inhibits glutamate
- weight gain
- can cause respiratory depression, especially with opioids or benzos
Diazepam
Lorazepam
Benzodiazepines / Anti-Epileptics
- positive allosteric modulators at GABAa
- for acute seizure attacks
- can develop tolerance
Phenobarbital
Barbiturate / Anti-Epileptic
- GABA agonist at high doses
- 1st line for neonatal seizures
Levetiracetam
SV2A Modulator (Anti-Epileptic)
- well tolerated broad spectrum anti-epileptic
Carbidopa / Levodopa
Dopamine Precursors (Parkinson’s)
- L-dopa passes BBB to increase DA
- Carbidopa reduces conversion of L-Dopa to DA
- used for basically all Parkinson’s pts
Sinemet
Dopamine Precursors (Parkinson’s)
- brand name for carbidopa / levodopa
Entacapone
L-Dopa/DA Degradation Inhibitor (Parkinson’s)
- COMT inhibitor
- causes orthostatic hypotension
Rasagiline
L-Dopa/DA Degradation Inhibitor (Parkinson’s)
- MAO-B inhibitor
- may be NEUROPROTECTIVE
Stalevo
L-Dopa/DA Degradation Inhibitor (Parkinson’s)
- Entacapone + Carbidopa / Levodopa
Pramipexole
DA Receptor Agonist (Parkinson’s)
- for younger pt, hallucinations in older pt
Rotigotine
DA Receptor Agonist (Parkinson’s)
- once daily patch
- can cause hyperhidrosis
Bromocriptine
DA Receptor Agonist (Parkinson’s)
- also 5HT inhibitor and glutamate inhibitor
- exacerbates/causes heart disease
Benztropine
Anticholinergic - ACh Inhibitor (Parkinson’s)
- inhibits DAT and ACh (an excitatory NT)
- can cause tachycardia or psychosis
Lidocaine
Local Anesthetic
- Amine
- degraded by cytochrome P450
- hepatotoxic
Bupivacaine
Local Anesthetic
- Amine
- degraded by cytochrome P450
- hepatotoxic
Benzocaine
Local Anesthetic
- Ester
- degraded by plasma esterases
- more likely to cause allergic reactions
Cocaine
Local Anesthetic
- Ester
- degraded by plasma esterases
- more likely to cause allergic reactions
Propofol
General Anesthetic
- enhances GABAa receptor
- induction and maintenance
- antiemetic
Ketamine
General Anesthetic
- NMDA receptor antagonist
- AWAKE AMNESIA
- bronchodilator that can cause bronchospasm
Midazolam
General Anesthetic
- positive allosteric modulator at GABAa
- shortest half life
Methohexital
General Anesthetic
- positive allosteric modulator at GABAa
Etomidate
General Anesthetic
- enhances GABAa
- CARDIOSTABLE, USE IN PT AT RISK FOR HYPOTENSION
- significant nausea and vomiting
Flumazenil
Used to shorten recovery from anesthesia with benzodiazepines
Isoflurane
General Anesthetic - Inhaled (Volatile)
- pungent odor
- tachycardia and malignant hypothermia
Sevoflurane
General Anesthetic - Inhaled (Volatile)
- induction and maintenance
- NOT IRRITATING TO AIRWAYS
- malignant hypothermia
Desflurane
General Anesthetic - Inhaled (Volatile)
- used to maintain anesthesia
- NO INDUCTION DUE TO AIRWAY IRRITATION
- tachycardia and malignant hypothermia
Nitrous Oxide
General Anesthetic - Inhaled (Volatile)
- weak anesthetic, used as adjunct
- can cause diffusion hypoxia, need to give 100% O2 at end of procedure
- IMPOTENT –> MAC = 105%
Morphine
Opioid
- Mu agonist
- can cause respiratory depression and constipation
Hydromorphine
Morphine-Like Opioid
- Mu agonist
- can cause respiratory depression and constipation
- preferred in renal pt
Fentanyl
Morphine-Like Opioid
- Mu agonist
- can cause respiratory depression and constipation
- no histamine release
Heroin
Morphine-Like Opioid
- Mu agonist
- can cause respiratory depression and constipation
Codeine
Opioid
- Mu agonist
- can cause respiratory depression and constipation
- metabolized by CYP2D6
- no patients <18 years old
Oxycodone
Codeine-Like Opioid
- Mu agonist
- can cause respiratory depression and constipation
- COMBINED WITH ACETAMINOPHEN = POSSIBLE ACETAMINOPHEN TOXICITY
Hydrocodone
Codeine-Like Opioid
- Mu agonist
- can cause respiratory depression and constipation
- COMBINED WITH ACETAMINOPHEN = POSSIBLE ACETAMINOPHEN TOXICITY
Tramadol
Opioid
- Mu agonist
- NET/SERT inhibitor
- LOW RISK of respiratory depression, constipation, or abuse
- can cause serotonin syndrome
Pentazocine
Opioid
- Kappa agonist, Mu antagonist
- causes dysphoria, increase HR and BP