Exam 2 but simplified Flashcards
Statins: Class, indications (1), MOA, AE (3), PK (3)
Class: HMG-CoA Reductase Inhibitors
Indications: High cholesterol blood lvl
MOA: Inhibits HMG CoA reductase → inc. LDL receptor proliferation → inc. LDL uptake into cell
AE: All rare, generally well tollerated
- Myopathy (rhabdomyolysis)
- Hepatotoxicity
- Renal injury
PK
- PO at night
- No grapefruit!
- Rosuvastatin is not well metabolized in Asian heritage
Colesevelam // Colestipol // Cholestyramine: Class, indications, MOA, AE
Class: Bile acid sequestrants
Indications: High cholesterol blood lvl
MOA: Nonabsorbable from GI tract → binds to bile acid → dec. reabsorption and inc. excretion of cholesterol
- Ultimately inc.s LDL receptors in the liver
AE: GI disturbance (constipation)
Ezetimibe: Indications, MOA, AE (4), PK
Indications: High cholesterol blood lvl
MOA: Act on brush border enzyme → prevents dietary cholesterol absorption and inhibits reabsorption of cholesterol secreted in the bile
AE:
- Myopathy (rhabdomyolysis)
- Hepatitis
- Pancreatitis
- Thrombocytopenia
PK: Converted to active metabolite ezetimibe glucuronide
Gemfibrozil // Fenofibrate: Class, indications, MOA, AE (4)
Class: Fibric acid derivatives (fibrates)
Indications: To lower VLDL levels
MOA: Inhibits hepatic extraction of free fatty acids → liver cannot synthesize as many triglycerides → dec. VLDL
AE: GI disturbances are most common
- Gallstones
- Myopathy
- Hepatotoxicity
Monoclonal antibody (PCSK9) inhibitor: Indications, MOA, AE (2), PK (2)
Indications: High cholesterol blood lvl
MOA: PCSK9 is a protein that binds LDL receptors in the liver
- Inhibition of PCSK9 = freed receptors = inc. LDL uptake
AE:
- Hypersensitivity
- Immunogenicity
PK: SubQ only
- Used with statins
ACL inhibitor: Indications, MOA, AE (2), PK
Indications: High cholesterol blood lvl
MOA: Inhibit ACL → dec. cholesterol synthesis → inc. LDL receptor proliferation → inc. LDL cell uptake
AE:
- Increase uric acid (gout risk)
- Increase tendon rupture risk
PK: Converted to active metabolite
Angiotensin-converting enzyme (ACE) inhibitors (-pril): Indications, MOA (5ish), AE (8), PK (3), Cont (2)
Indications: HTN
MOA: Inhibits ACE = Inhibition of ANG2 formation
- Inc. vasodilation
- Inc. diuresis, excrete out more Na
- Dec. SNS response = dec. myocardial O2 supply
- Prevention of CV remodeling
AE:
- HypoTN (first dose especially)
- HyperK
- Dehydration
- Cough
- Fetal injury
- Renal failure
- Rare: Angioedema, neutropenia
PK: PO (except enalapril, which is IV)
- All prodrugs (except lisinopril) that are converted in small intestine
- Long 1/2 life
Contraindications:
- Drugs that exacerbate hypotension or K+ levels
- Pregnancy
Angiotensin II receptor blockers (ARBs) (-artan): Indications, MOA, AE (6), PK
Indications: HTN
MOA: Blocks the effects of ANG2 at the receptor
- Inc. vasodilation
- Inc. diuresis, excrete out more Na
- Dec. SNS response = dec. myocardial O2 supply
- Prevention of CV remodeling
AE:
- HypoTN
- HyperK (low)
- Dehydration
- Cough (low)
- Fetal injury
- Renal failure
PK: All PO
Aliskiren: Class, indications, MOA (5ish), AE (6)
Class: Direct renin inhibitor
Indications: HTN
MOA: Inhibit release of renin = block entire RAAS
- Inc. vasodilation
- Inc. diuresis, excrete out more Na
- Dec. SNS response = dec. myocardial O2 supply
- Prevention of CV remodeling
AE:
- HypoTN
- HyperK
- Dehydration
- Cough, angioedema
- Fetal injury
- Diarrhea
Nifedipine: Class, indications (2), MOA (3), AE (5), Cont
Class: Ca channel blockers
- Dihydropyridines
Indications:
- Prinzmetal angina
- HTN
MOA: Blocks Ca2+ vascular smooth muscle
- Vasodilation of coronary arteries
- Dec. afterload
- Inc. contractility
AE:
- Peripheral edema
- Flushing
- Dizziness
- Headache
- Inc. myocardial O2 demand
Cont: No beta blockers
Verapamil // Dilitiazem: Class, indications (4), MOA, AE (6), cont (3)
Class: Ca channel blockers
- Non-dihydropyridines
Indications:
- HTN
- Angina
- Dysrhythmias
- SVT
MOA: Blocks Ca2+ @ vascular smooth muscle and the heart
- Dec. HR, contractility, AV node conduction
- Artery vasodilation → decrease afterload, coronary artery vasoconstriction
AE:
- Constipation
- Flushing, dizziness, headache
- Edema
- Bradycardia
- Heart block
- Hypotension
Contraindications:
- BB and Digoxin
- HF
Hydralazine: Class, indications, MOA, AE (5)
Class: Vasodilator
Indications: HTN
Actions: Dec. afterload
MOA: Unknown
- Direct arteriole vasodilation
AE:
- Fluid retention with long-term use
- Headache
- Dizziness
- Hypotension
- Reflex tachycardia
Sodium nitroprusside: Class, indications, MOA, AE, PK
Class: Vasodilator
Actions: Dec. preload
Indications:
- Prinzmetal angina
- HTN
MOA: Vasodilate veins via NO
AE: Tolerance can develop rapidly
PK: PO has insane first pass effect
Nitroglycerin: Class, indications, MOA, AE, Cont (4)
Class: Organic nitrates
Indications: HTN
- Angina
MOA: Converted to NO = NO activated guan = guan catalyzes cGMP = cGMP inhibits light chain = relax, vasodilation
AE: Tolerance
Contraindications:
Other hypotensive drugs + nitrates (ex: PDE5 inhibitors)
BB, CBB, diuretics
Digoxin: Class, indications, MOA, AE (5), Cont (4)
Class: Cardiac glycoside
Indications: HTN
MOA: Selectively inhibits Na/K/ATPase pump
- Build up of Ca2+ intracellularly = inc. actin/myosin interactions
AE: Heart dysrhythmia
GI: Anorexia + N/V (she’s so mean she causes bulimia)
CNS: Fatigue + visual disturbances
Contraindications:
Heart block
Bradycardia
Renal impairment
Electrolyte disturbances
Furosemide: Class, indications, MOA, AE (5), Cont (2)
Class: Loop Diuretics
Indications: HTN
MOA: Blocks Na/Cl/K cotransporter in ascending LoH → excrete Na+/K+/2Cl- in urine followed by water
AE:
- HypoK
- HypoNa+
- HypoCl-
- Ototoxicity
- Dehydration/hypotension
Contraindications:
Other ototoxic drugs (aminoglycoside antibiotics)
Digoxin
Hydrochlorothiazide (HCTZ): Class, indications, MOA, AE (6)
Class: Thiazide Diuretics
MOA: Block Na/Cl/K reabsorb @early distal convoluted tubule → these are excreted in urine followed by water
AE:
- HypoK
- HypoNa+
- HypoCl-
- Dehydration/hypotension
- Increase uric acid lvl (gout risk)
- Ineffective in kidney disease
Spironolactone: Class, indications, MOA, AE (3)
Class: K+ Sparing Diuretics
MOA: Blocks aldosterone
- Decrease prod of Na/K exchange protein transporter
- K+ retention, Na+/H2O excretion @late distal convol tubule
- Dec. remodeling of CV system
AE:
- HyperK
- Endocrine: Menstrual irregularities, gynecomastia
Mannitol: Class, indications, MOA, AE (2)
Class: Osmotic Diuretics
MOA: Freely filtered in GFR, stays in filtrate → draw water out to be excreted in urine
AE: Fluid overload/edema
- HF
Heparin // LMWH: Class, indications (5), MOA, AE
Class: Antithrombin activator
Indications:
- DVT/PE
- Open heart surgery
- Dialysis
- Disseminated intravascular coagulation (DIC)
- Acute MI
MOA: Activate antithrombin → inhibit coagulation factors to prevent
AE: Hemorrhage/bleeding
Warfarin: Class, indications (3), MOA, AE, PK (3)
Class: Vitamin K inhibitor
Indications:
- DVT/PE
- Thromboembolism in prosthetic heart valves
- MI/stroke risk
MOA: Inhibits enzyme that activates vitamin K → prevents synthesis of factors 2, 7, 9, 10 → dec. fibrin formation
AE: Hemorrhage/bleeding
PK:
- 99% protein bound
- Free drug crosses membranes (placenta, breastmilk)
- CYP450 hepatic metabolism
Dabigatran // Bivalirudin // Desirudin // Argatroban: Class, indications (2), MOA, AE (2), PK (2)
Class: Direct thrombin inhibitors
Indications: Prevent thrombosis
- DVT/PE
MOA: Inhibit thrombin → dec. conversion of fibrinogen to fibrin and activation of factor XIII → prevents fibrin mesh formation
AE: GI upset
- Hemorrhage/bleeding
PK:
- Food affects absorption rate
- Low protein binding
Rivaroxaban: Class, indications (3) , MOA, AE, cont
Class: Direct factor Xa inhibitors
Indications:
- DVT/PE
- Prevent thrombosis
- CVA
MOA: Inhibit factor 10a → prevent fibrin mesh formation
AE: Hemorrhage/bleeding
Cont: Pregnancy
Asprin: Class, indications (5), MOA, AE, PK
Class: COX inhibitor (irreversible)
Indications:
- Acute MI
- CVA
- TIA
- Chronic stable angina
- Stents
MOA: Inhibit COX → dec. platelet activation/aggregation, dec. TXA2 mediated vasoconstriction → inhibit platelet plug
AE: Hemorrhage/bleeding
PK: Effects last the lifetime of platelet
Clopidogrel // Prasugrel // Ticagrelor: Class, indications, MOA, AE (2), PK (3)
Class: P2Y12 ADP receptor antagonists
Indications: Prevention of stent thrombosis & thrombotic events
MOA: Antagonize P2Y12 receptor so ADP can’t bind → dec. platelet activation/aggregation → inhibit platelet plug
AE: Hemorrhage/bleeding
Vorapaxar: Class, indications, MOA, AE, PK
Class: PAR-1 antagonist
Indications: Use with aspirin/clopidogrel in reduction of thrombotic events
MOA: Reversible binding to PAR-1 receptors on platelet surface → dec. effects of thrombin → dec. platelet activation/aggregation
AE: Bleeding/hemorrhage
PK: Long half life
Abciximab: Class, indications, MOA
Class: GP IIb/IIIa receptor antagonists
Indications: Short term to prevent ischemic events in those w/ ACS or undergoing PCI
MOA: Blocks IIb/IIIa receptors on platelet inhibition of final
common step in platelet aggregation
- Inhibits aggregation from all factors (collagen, TXA2, ADP, thrombin,
platelet activation factor)
Alteplase (tPA) // Tenecteplase // Reteplase: Class, indications, MOA, AE
Class: Thrombolytic drugs
Indications: Remove already formed clots
- Acute MI
- Acute stroke
- Acute massive PE
MOA: Binds to plasminogen -> plasmin
- Plasmin breaks down already-formed clot
AE: Special handling
Quinidine // Procainamide: Class, indications, MOA (3), AE
Class: IA antidysrhythmic
- Na+ channel blocker
Indications: Atrial and ventricular arrhythmias
MOA: Blocks Na+ channel
- Inc. AP
- Inc. ERP
- Inc. QT interval
AE: Anticholinergic (inc HR)
Lidocaine: Class, indications (2), MOA (2), AE
Class: IB antidysrhythmic
- Na+ channel blocker
Indications:
- Post MI
- Ventricular arrhythmias
MOA: Blocks Na+ channel
- Dec. AP
- Dec. ERP
AE: Toxicity at high doses
IC antidysrhythmics: Class, indications (2), MOA, AE
Indications:
- SVTs
- Afib
MOA: Blocks Na+ channel
- Inc. ERP in AV node (but not ventricular tissue)
AE: Can induce life-threatening VT
Metoprolol // Esmolol: Class, indications (3), MOA (3), AE (3)
Class: Beta blockers
Indications:
- SVT
- VT
- Post-MI
MOA: Dec. HR, contractillity, AV node conduction
AE:
- Bradycardia
- HypoTN
- Can’t be given with CCB
Amiodarone: Class, indications, MOA (4), AE (8), PK
Class: K+ channel blocker
Indications: VT
MOA: Blocks K channel
- Delay repolarization
- Inc. AP duration
- Inc. ERP
- Prolongs QT
AE:
- Pulmonary fibrosis
- Hypothyroidism
- Hepatotoxicity
- Prodysrhythmic: torsades, bradycardia, AV block
- Corneal microdeposits
- Skin discoloration
PK: Extremely long half life (25-60 days)
Adenosine: Class, indications, MOA, AE (4), PK
Class: Class V antidysrhythmic
Indications: VT
MOA: Binds adenosine receptor in cardiac tissue → open K+ channel → hyperpolarize → prevent next contraction / temporary heart stop
AE:
- Flushing
- Transient hypotension
- Transient chest pain
- Transient flat line
PK: Extremely short half life (10 secs) → needs to be given w saline flush
Atropine: Class, indications, MOA, AE (3)
Class: Anti-cholinergic
Indications: Symptomatic bradycardia
MOA: M antagonism
- Inc. HR
AE:
- Decreased GI/GU activity
- Mydriasis
- Dry mouth
Disulfram: Uses (1), AE (12)
Use: Unpleasant rxn w/ alcohol (abstinence)
AE:
- Nausea
- Vomiting
- Palpitations
- Weakness
- Blurry vision
- Hypotension
- Dysrhythmias
- MI → CV collapse
- Respiratory depression
- Convulsions
- Death
Naltrexone: Uses, MOA (2), AE (4)
Use: Dec craving (“most effective”)
MOA: blocks “fun” effects of alc, blocks opioid euphoria
AE:
- Nausea
- Headache
- Dizziness
- Sedation
Acamprosate: Use
Blocks some bad abstinence feelings
Nicotine replacement therapy: MOA, Types (5) + their MOAs (5)
MOA: plasma nicotine rises slowly → less pleasure
Types + their MOA:
- Gum + lozenge: oral mucosa → systemic circulation
- Patch: steady plasma nic concentration
- Inhaler: looks like cig
- Nasal: level rises quickly but w/o toxic chemicals
Buproprion: Use (2), AE (4), Contraindications (2)
Use: Reduce nicotine cravings, lessen withdrawal symptoms
AE:
- Dry mouth
- Insomnia
- Headache
- Seizures
Contraindications:
- Seizures with alcohol
- MAOI use
Varencline: Use (1), MOA (3), AE (6)
Use: Nicotine abstinence
MAOI:
- Block pharmacological effects of nicotine
- Promote dopamine release
- Partial NAChR agonist
AE:
- Headache
- Nausea
- Constipation
- Dry mouth
- Taste change
- Flatulence
Methadone: Class, MOA (1), Special (1)
- Class: opioid substitute
- MAOI: substitute with longer 1/2 life → less euphoria
- Special: higher dose to increase tolerance → street opioid doesn’t work
Buprenorphine: Class, MOA, Uses (3)
Class: Opioid agonist-antagonist
MAOI: Mu agonist, kappa antagonist
Uses:
- Alleviate cravings
- Reduce use
- Ceiling to respiratory depression (SAFER)
Naloxone (Narcan): Class, DOA, MOA
Class: opioid antagonist
DOA: 1hr
MOA: Antagonist mu + kappa
Flumazenil: Class, MOA, Use (2)
Class: Benzo abstinence
MOA: Reverse sedation
Use:
- Taper
- Less withdrawal symptoms
Marijuana: MOA (4), Indications (5)
MOA:
- THC lipid soluble
- Rapid absorption via inhalation
- CYP450 inhibitor
- Cannabinoid receptor activity in the brain
Indications:
- Suppress emesis (cancer)
- Stimulate appetite in AIDs pts
- Seizures
- Neuropathic pain
- Various unapproved
Levodopa: Uses (1), Special (5), AE (6), Contraindications (1)
Uses: Severe PD → most effective
Special:
- Effects diminish over 5 years
- Prodrug → needs to convert to dopamine
- Needs help crossing BBB
- Need COMT inhibitor + decarboxylase inhibitor
- Don’t eat high-protein meals
AE:
- Nausea/vomiting
- Dyskinesia
- Post-orthostatic hypotension early
- Dysrhythmia risk
- Psychosis
- Anxiety
Contraindication: MAOIs (severe HTN)
Carbidopa: MOA, Special (3)
MOA: decarboxylase inhibitor
Special:
- Take WITH Levodopa
- NO effects on own
- NO crossing BBB
Entacapone: MOA, Special (3)
MOA: COMT inhibitor
Special:
- Take WITH Levodopa
- Dec peripheral AE
- NO effects on own
Pramipexole, Ropinirole, Rotigotine: Class (2), Use, AE (5), Special (2)
Class:
- Dopamine selective agonist
Use: mild-moderate PD
AE:
- Nausea/vomiting
- Dizziness
- Constipation
- Weakness
- Hallucinations
Special:
- NO dyskinesia
- DO NOT take 5-HT antagonists (orthohypo) or dopamine receptor antagonists (opp effect) if N/V
Apomorphine: Class (2), Use, Special (2), AE (6)
Class:
- Dopamine agonist
- Nonergot alkaloid
Use: Hypomobile episodes
Special:
- NO PO
- Morphine derivative
AE:
- Injection site rxn
- Hallucination
- Drowsiness
- Dyskinesia
- Nausea/vomiting
- Serious CV events
Selegiline: Class, Use, AE (5), Interactions (4)
Class: Irreversible MAO-B binding
Use: FIRST LINE mild-moderate PD
AE:
- HTN (MAO-A binding @ high dose)
- Orthostatic hypotension
- Dizziness
- GI excite
- Insomnia
Interactions
- Intensify Levodopa
- Increase AE of opioids
- Serotonin syndrome risk (opioids)
- Serotonin syndrome risk (SSRIs)
Rosagiline: Class, Use, AE (4), Interactions (4)
Class: Irreversible MAO-B binding
Use: FIRST LINE mild-moderate PD
AE:
- HTN (MAO-A binding @ high dose)
- Orthostatic hypotension
- Dizziness
- Malignant melanoma
Interactions
- Intensify Levodopa
- Increase AE of opioids
- Serotonin syndrome risk (opioids)
- Serotonin syndrome risk (SSRIs)
Amantadine: MOA, Use, AE (5)
MOA: Increase dopamine
Use: help with dyskinesia via Levodopa
AE:
- Confusion
- Dizziness
- Anxiety
- Peripheral effects
- Mottled discoloration (>1 mo use)
Benzotropine: Class, Use, MOA, AE (4)
Class: Anticholinergic
Use: 2nd line for tremors
MOA: Block M receptors
AE:
- Sedation
- Confusion
- Hallucination
- Peripheral AEs
Donepezil: Class (2), Special (1), AE (3), Contraindications (2)
Class:
- Reversible AChE inhibitor
- Selective for CNS but some PNS
Special: Long 1/2 life (70hr) + time to plateau (15d)
AE:
- Peripheral chole effects
- Bradycardia
- Heart block
Contraindications
- COPD
- Anticholinergics
Rivastigmine: Class (2), AE (3), Contraindications (2)
Class:
- Irreversible AChE inhibitor
- More PNS than CNS
AE:
- Peripheral chole effects
- Bradycardia
- Heart block
Contraindications
- COPD
- Anticholinergics
Galantamine: Class (1), AE (3), Contraindications (2)
Class: Reversible AChE inhibitor
AE:
- Peripheral chole effects
- Bradycardia
- Heart block
Contraindications
- COPD
- Anticholinergics
Memantine: Class (1), Special (2), Drug interaction (1)
Class: NDMA receptor antagonist
Special:
- Minimal AE
- Allows normal cell signaling
Interaction: Other NDMA blockers (ketamine, amantidine)
Interferon beta: Class (1), Use, AE (9), Special (1)
Class: Immunomodulator
Use: MS
AE:
- Hypersensitivity rxn
- Neutralize antibody production
- Infection
- Hematological changes
- Liver injury
- Decrease vaccine responsiveness
- Flu-like rxn
- Depression
- Injection site rxn
Special: Pregnant RNs handle with care!
Mitoxantrone: Use, Class (1), MOA (1), AE (4)
Use: MS
Class: Immunosuppressant
MOA: Inhibit DNA synthesis/repair → dec demyelination
AE:
- Myelosuppression (all -nias)
- Irreversible cardiotoxicity → heart failure
- Fetal injury
- Cancer + infection
Dalfampridine: Class (1), Use (1)
Class: K+ channel blocker
Use: Gait issues
Traditional anti-seizure drugs: overall
LOTS of AEs and drug interactions
Penytoin: MOA, Type, AE (6), Special (1), Drug interactions (3)
MOA: Selective Na+ channel inhibitor on HYPERACTIVE neurons
Type: Traditional anti-seizure medication
AE:
- CV effects (DILUTE to avoid)
- CNS depression
- Gum issues
- Skin issues
- Teratogen
- Necrosis w/ extravasation
Special: High toxicity risk → monitor dose
Interactions:
- Decreases the effects of other drugs
- Affected by CYP450 inhibitors/inducers
- Avoid with other CNS depressants
Fosphenytoin: Type (2), MOA
Type: prodrug, traditional antiseizure med
MOA: converts to penytoin
Carbamazepine: MOA, Type, AE (4), MOA (1)
MOA: Selective Na+ channel inhibitor on HYPERACTIVE neurons
Type: Traditional anti-seizure medication
AE:
- CNS depression
- Bowel movement suppression
- H2O retention
- Skin issues
MOA: Metabolized by + induces CYP450
Valproate: MOA, Type, AE (6), Drug Interaction (1)
MOA: Enhance GABA transmission + Na+ block
Type: Traditional anti-seizure medication
AE:
- Life-threatening pancreatitis
- Fetal liver failure
- Teratogen
- Weight gain
- Hair loss
- Tremors
Interaction: DON’T combine with other antiseizure drugs → CNS depression
Ethosuximide: Use (1), Type, MOA, Special (1)
Use: Absence seizures
Type: Traditional anti-seizure medication
MOA: Suppress Ca+ channels
Special: Minimal AE
Phenobarbital: MOA, Type, Special (2), AE (4)
MOA: Potentiate GABA effects (Direct receptor agonist)
Type: Traditional anti-seizure medication
Special:
- Long 1/2 life (4 days)
- Used for anesthesia
AE:
- CNS depression
- Acute intermittent porphyria
- Vitamin D metabolism interference
- Physical dependence
Oxcarbazepine: MOA, Type, AE (5), Drug interactions (4)
MOA: Na+ channel inactivation
Type: New-gen anti-seizure meds
AE:
- CNS depression
- Hyponatremia
- Hypothyroidism
- Skin issues
- Hypersensitivity
Interactions:
- Other antiseizure medication
- CYP450 inducer
- Avoid alcohol
- Avoid other hyponatremic drugs
Lamatrigine: MOA (2), Type, AE (1), Contraindication (1)
MOA:
- Na+ channel inactivation
- Ca+ channel blockage
Type: New-gen anti-seizure meds
AE: Suicidal ideation (?)
Contraindication: Estrogen decreases levels (OC)
Gabapentin: MOA, Type, Special (1)
MOA: Enhance GABA release (?)
Type: New-gen anti-seizure meds
Special: Well tolerated
Pregabalin: MOA (3), Type, AE (3)
MOA:
- Bind Ca+ presynaptically
- Inhibit glutamate
- Inhibit norepinephrine
Type: New-gen anti-seizure meds
AE:
- Hypersensitivity
- Euphoria
- Decreased fertility
Levetiracetam: Type, AE (1)
Type: New-gen anti-seizure meds
AE: Maybe renal injury?
Topiramate: MOA (3), Type, AE (2), Drug interaction (1)
MOA:
- Na+ block
- Ca+ block
- Glutamate receptor block
Type: New-gen anti-seizure meds
AE:
- Metabolic acidosis
- Increase suicidal ideation
Interaction: Penytoin
Tiagabine: MOA (1), Type
MOA: Dec GABA reuptake
Type: New-gen anti-seizure meds
Baclofen: Use (1), MOA (1), AE (5), Contraindications (3)
Use: Muscle spasticity
MOA: Mimics GABA @ synaptic cleft (does NOT decrease muscle strength)
AE:
- CNS depression
- OD→ coma + respiratory depression
- Nausea/vomiting
- Constipation
- Withdrawal symptoms
Contraindications:
- CNS depressants
- Urinary retention
- Psych conditions
Dantrolene: Use (1), MOA (1), AE (4), Contraindication (1)
Use: Muscle spasticity
MOA: Decrease Ca+ effux from the sarcoplasmic reticulum
AE:
- Decrease strength/function
- Hepatic toxicity
- Drowsiness
- Diarrhea
Contraindication:
- CCB
Cyclobenzaprine: Use (1), MOA (1), AE (2), Drug interactions (2)
Use: Muscle spasms
MOA: Acts on brainstem to motor neuron pathways
AE:
- CNS depression
- Cardiac rhythm changes
Interactions:
- Serotonin syndrome risk (MAOIs, TCAs, SSRIs, SNRIs)
- CNS depression with depressants (alcohol
2 types of localized anesthetics + what metabolizes them
Esters: plasma esterase
Amides: hepatic enzymes
Chloroprocaine, Benzocaine: Class, MOA (1), AE (8), Special (1)
Class: Ester
MOA: Block Na+ channels
AE:
- CNS excitation → CNS depression
- Bradycardia
- Heart block
- Decrease contractility
- Cardiac arrest
- Vasodilation
- Allergic rxn
- Fetal toxicity (ion trapping)
Special: AVOID IV injection for nerve blocks
Methemoglobinemia: MOA
Convert Hgb → MetHgb (can’t carry O2)
Cocaine: Class, MOA (2), Contraindications (1)
Class: Ester
MOA:
- Block Na+ channels
- Block NE reuptake
Contraindications: Any CV disease
Lidocaine: Class, MOA, Administration (3)
Class: Amide
MOA: Block Na+ channels
Administration:
- Topical
- IV
- Injection
General anesthesia: General indication (1), Special (1)
General indication: Loss of consciousness → decreased response to painful stimuli
Special: Does NOT imply pain relief
Propofol: MOA (3), AE (6), Onset time
MOA:
-Enhance GABA → hyperpolarization → hard to get an AP
- Inc CNS depression
- Low dose for sedation, high for anesthetic
AE:
- Apnea
- Hypotension
- Reflex tachycardia
- Reflex bradycardia
- Injection site pain
Onset time: <60sec
Ketamine: MOA (2), Indications (2), AE (2)
MOA:
- Dec NMDA transmission
- Dec CNS excitation
Indications:
- Analgesia
- Dissociative anesthesia
AE:
- Hallucinations → maintain peaceful environment
- Bad dreams
Inhalation general anesthesia: AE (5)
Respiratory depression
- Cardiac depression
- Sensitive the myocardium to catecholamines → dysrhythmias
- Nausea/vomiting post-op
NSAIDs: MOA (1), Actions (9)
MOA: COS inhibiters dec COS activity → dec conversion of arachidonic acid to prostaglandins, prostacyclin, TXA2
Actions:
- Dec inflammation
- Dec pain receptor sensitivity
- Inc gastric acid secretions
- Dec platelet aggregation
- Dec vasodilation
- Dec vasodilation of renal artery
- Mediate fever
- Dec perception of pain
- Dec long-term uterine contractions
Aspirin, Ibuprofen: MOA (2), Indications (5), AE (5), Contraindications (4), Drug Interactions (4)
MOA:
- Nonselective COX inhibitor (1st gen)
- Aspirin irreversible binding → high levels of inhibiting platelet aggregation
Indications:
- Suppress inflammation
- Analgesia of mild-mod pain
- Fever reduction
- Suppress platelet aggregation
- Cancer prevention (colorectal)
AE:
- GI effects
- Renal impairment
- Reye syndrome
- Toxic to fetus
- Hypersensitivity rxn
Contraindications:
- Bleeding disorder
- Propensity for bleeding
- Children
- Pregnancy
Drug interactions:
- Anticoagulants → inc bleeding
- Glucocorticoid → gastric ulcers
- ARBS/ACEi → renal impairment
- Vaccines → suppress immune response
Celecoxib: MOA, Indications (3), Special (2), AE (3), Contraindications (2)
MOA: Selective COX-2 (2nd gen)
Indications:
- Rheumatoid arthritis
- Ankylosing spondylitis
- Acute pain
Special:
- Less AE due to dec inhibition of “good” COX
- No suppression of platelet aggregation + inhibiting vasodilation
AE:
- GI ulcer (low)
- Renal impairment
- Biggest concern: CV events
Contraindications:
- Heart disease
- Coronary artery bypass
Acetaminophen: MOA (2), Indications (5), Special (3), AE (4)
MOA:
- COX inhibitor
- NOT NSAID
Indications:
- Pain relief + fever
- NO anti-inflammatory
- NO platelet aggregation suppression
- NO GI disturbance
- NO change in renal blood flow
Special:
- Only works in CNS
- Major metabolization CYP450 oxidation
- @ high doses: run out of glutathione → toxic metabolite accumulate + liver damage
AE:
- OD → liver dmg (4g/day MAX)
- NVD
- Sweating
- Hepatic injury