KISS B2 Flashcards
Prils
Lisinopril & Ramipril (big 2)
Increased Bradykinin
Increased Angiotensin 1
Reduced Angiotensin 2
Reduced Aldosterone
Reduced K+
Reduced Renin
Rx:
HR & HTN
AE:
CATCHH
Cough
Angioedema
Teratogen
Hyperkalemia
Hypotension
Prils
Lisinopril & Ramipril (big 2)
Inhibit ACE:
Increased Bradykinin
Increased Angiotensin 1
Reduced Angiotensin 2
Reduced Aldosterone
Reduced K+
Reduced Renin
Rx:
HR & HTN
AE:
CATCHH
Cough
Angioedema
Teratogen
Hyperkalemia
Hypotension
5-lipooxygenase inhibitor
Prevents conversion of arachidonic acid into 5-hydroperoxide (& then leukotrienes)
Rx Severe asthma
AE:
Hepatotoxicity/Hepatitis
Zilueton
Rx Myasthenia gravis & Cobra venom use
Neostigmine & Pyridostigmine
Blurry yellow vision
Arrythmias
AV block
Diarrhea
Indicate which toxicity? & what is the antidote?
Digoxin toxicity treated with digoxin anti-FABS
Activated receptors on precursor RBC’s to stimulate erythropoiesis
Rx Anemia or avoid anemia in transfusions
AE:
Thrombotic events & HTN
EPO
B-blocker
MOA:
Blocks norepinephrine’s action at the ciliary epithelium without causing pupil or vision changes
Effects:
1) Reduced aqueous humor production (blocks B2 receptors)
Describes which drug
Timolol
Heavy bleeding & skin necrosis
What is the toxicity & the antidote
Warfarin toxicity
Rx Vitamin K & Fresh frozen plasma
PDE-5 inhibitor causing more cGMP to generate NO causing vasodilation & pulmonary artery relaxation
Sildenafil
B agonist that targets B1 & B2 receptors equally
MOA:
It activates Gs to increase adenylate cyclase & cAMP resulting in more norepinephrine release to bind to B receptors (dilation)
Effects:
1) Increased cardiac output
2) Increased heart rate
3) Reduced BP
Clinical uses:
1) Bradycardia
2) Heart block (AV)
3) Cardiac arrest
Adverse effects:
1) Tachycardia
2) Arrythmia
Describes which drug?
Isoprotenolol
Classification: PGE1 analog
Mechanism of Action: relaxes smooth muscle in ductus arteriosus
Clinical Indications: maintains patency of ductus arteriosus, impotence
Adverse Effects: hypotension, N/V/D, vaginal bleeding, uterine cramping, flushing tachycardia
Alprostadil
Mechanism of Action: PGE1 analog –– increase production and secretin of gastric mucous barrier and decreased acid production
Clinical Indications: prevention of NSAID-induced peptic ulcers, off label use for labor induction (ripens cervix)
Adverse Effects: N/V/D, hypotension, potential abortifacient (contraindicated of women of childbearing potential), vaginal bleeding, uterine cramping, flushing tachycardia
Misoprostol
Mechanism of Action: reversibly inhibits cyclooxygenase – mostly in CNS –– inactivated peripherally –– lacks significant anti-inflammatory effects
Clinical Indications: antipyretics, analgesic (act on cannabinoid receptor)
Adverse Effects: hepatic necrosis (overdose)
Acetaminophen
Classification: non-steroidal anti-inflammatory
Mechanism of Action: reversibly inhibit COX-1 and COX-2 –– blocks prostaglandin synthesis
Clinical Indications: antipyretic, analgesics, anti-inflammatory –– close PDA
Adverse Effects: interstitial nephritis, gastric ulcer, renal ischemia, aplastic anemia
Indomethacin
Classification: anti-gout
Mechanism of Action: binds and stabilizes tubulin to inhibit microtubule polymerization, impairing neutrophil chemotaxis and degranulation –– decrease LTB4 and decreases leukocyte and granulocyte migration
Clinical Indications: acute and prophylactic (acute gout drug)
Adverse Effects: diarrhea, acute GI pain, hematuria, alopecia, myelosuppression, gastritis, peripheral neuropathy (long-term use)
Colchicine
Classification: uricosuric –– anti-gout
Mechanism of Action: inhibition of renal reabsorption or uric acid
Clinical Indications: chronic gout
Adverse Effects: precipitate uric acid calculi, nephrotic syndrome, aplastic anemia, allergy
Contraindicated in acute gout
Sulfinpyrazone
Classification: anti-gout
Mechanism of Action: inhibits reabsorption of uric acid in PCT –– also inhibits the secretion of penicillin
Clinical Indication: prophylactic (chronic gout drug)
Adverse Effects: precipitate uric acid calculi, nephrotic syndrome, aplastic anemia, allergy
Contraindicated in acute gout
Probenecid
Classification: ergot alkaloid
Mechanism of Action: acts as partial agonist at both and 5HT2 receptors in the vasculature and possibly CNS –– vasoconstrictive actions to decrease pulsation in cerebral vessels
Clinical Indications: acute migraine attacks
Adverse Effects: GI distress, prolonged vasoconstriction can lead to ischemia and gangrene – abortion near term
Ergotamine
Classification: triptan
Mechanism of Action: 5-HT1B/1D agonists –– inhibit trigeminal nerve activation, prevent vasoactive peptide release, induce vasoconstriction
Clinical Indications: acute migraine, cluster headache attacks
Adverse Effects: coronary vasospasm (contraindicated with CAD and vasospastic angina), mild paresthesia, serotonin syndrome
Sumatriptan
Presentation: bleeding, skin necrosis (if low protein C)
Warfarin Toxicity
Antidote: fresh frozen plasma (acute), vitamin K (non-acute)
Presentation: bleeding
Heparin Toxicity
Antidote: protamine sulfate (positively charged molecule that binds negatively charged heparin)
Predisposing Factors: renal failure (decreased excretion), hypokalemia, drugs that displace digoxin from tissue-binding sites, and decreased clearance
Worsening Factors: hypokalemia, hypomagnesemia, hypercalcaemic
DIGOXIN POISONING
Antidote: slowly normalize K+, antiarrhythmics (lidocaine, phenytoin), cardiac pacer (severe), anti-digoxin Fab fragments, Mg2- –– propranolol and atropine (block vagus)
Pathogenesis: toxic doses cause respiratory alkalosis early, but transitions to mixed metabolic acidosis-respiratory alkalosis
Presentation: confusion, lethargy, ataxia, nystagmus, stupor, coma, hypothermia, respiratory failure
Aspirin/ Salicylates Poisoning
Sodium bicarbonate
Pathogenesis: acetaminophen metabolite (NAPQI) depletes glutathione and forms toxic tissue by-products in liver –– hepatic necrosis
Presentation: mild anorexia, N/V, delayed jaundice, hepatic and renal failure
Acetaminophen toxicity
Antidote: N-acetylcysteine (replenishes glutathione)
Precipitating Factors: consumption of deadly nightshade berries
Presentation: tachycardia, hypertension, hyperthermia (hot, dry skin), delirium, hallucinations, mydriasis
Atropine OD rx physostigmine
Presentation: severe GI distress leading to necrotizing gastroenteritis with hematemesis and blood diarrhea, dyspnea, shock and coma –– typically seen in children who have ingested iron tablets
Iron poisoning
Antidote: deferoxamine, deferasirox, deferiprone (Iron chelators) as well as gastric aspiration and carbonate lavage
Classification: low-molecular weight heparin
Mechanism of Action: bind ATIII –– have same inhibitory effect on factor Xa as the unfractioned heparin-ATIII complex –– longer half-life than standard heparin
Clinical Indications: anticoagulation –– does not need laboratory monitoring (more predictable mechanism of action)
Adverse Effects: same as heparin, but less likely to experience thrombocytopenia and thrombosis
Contraindicated in renal failure
Enopaparin (LWMH)
Predisposing Factors: commonly used as insecticides (poisoning usually seen in farmers)
Pathogenesis: OP irreversibly inhibit AChE
Organophosphate Poisoning
Antidote: atropine (antagonizes the actions at muscarinic receptor sites) and pralidoxime (regenerates AChE via dephosphorylation if given early)
3 Drugs that block ADP receptor to reduce GpIIB/IIIa EXPRESSION
Anti-inflammatory & antiplatelet
AE: Neutropenia & TTP
Clopidogrel, Prasugrel, Ticlopidine
Mechanism of Action: activates antithrombin III, which decreases action of IIa (thrombin) and factor Xa –– also IXa, Xia, XIIa and kallikrein(intrinsic and common pathways) –– short half-life –– conformational change in antithrombin that makes reactive site more accessible to proteases
Clinical Indications: immediate anticoagulation for PE, acute coronary syndrome, MI, DVT –– used during pregnancy (does not cross the placenta) –– follow PTT
Adverse Effects: bleeding, thrombocytopenia (non-immune and immune), osteoporosis, drug-drug interaction (warfarin), hyperkalemia
Contraindicated in patients with: hypersensitivity, active bleeding, active TB, threatened abortion, hemophilia, advanced hepatic/ renal disease, GIT ulcers, significant thrombocytopenia, purpura, severe hypertension, intracranial hemorrhage, infective endocarditis
Heparin
Classification: erythropoiesis-stimulating agent
Mechanism of Action: agonist of erythropoietin receptors expressed by red cell progenitors
Clinical Indications: anemias especially in chronic renal failure, HIV infection, cancer, prematurity –– prevention of need for transfusions
Adverse Effects: hypertension, thrombotic complications, pure red cell aplasia
Epoetin alfa (Erythropoietin)
Classification: Vitamin B12
Mechanism of Action: cofactor required for essential enzymatic reactions that form tetrahydrofolate, convert homocysteine to methionine, and metabolize L-methyl malonyl-CoA
Clinical Indications: vitamin B12 deficiency (megaloblastic anemia), basis of pernicious anemia
Cyanocobalamin
Mechanism of Action: precursor of an essential donor of methyl groups used for synthesis of amnio acids, purines and deoxynucleotides
Clinical Indications: folic acid deficiency (megaloblastic anemia), prevention of congenital neural tube defects
Adverse Effects: can mask vitamin B12 deficiency in large amounts
Folic Acid
Classification: megakaryocyte growth factor
Mechanism of Action: recombinant form of an endogenous cytokine –– activates IL-11 receptors –– stimulates the growth of primitive megakaryocytic progenitors and increases the number of peripheral platelets
Clinical Indications: secondary prevention of thrombocytopenia in patients undergoing cytotoxic chemotherapy for non-myeloid cancer
Adverse Effects: fatigue, headache, dizziness, anemia, fluid accumulation in the lungs, transient atrial arrythmias
Oprelvekin (IL-11)
Anti HTN safe in pregnancy?
Hydralazine
Labetolol
Methyldopa
Nifedipine
Amlodipine, Clevidipine, nicardipine, nimodipine
Ca channel blockers (class4 antiarrhythmics)
All treat raynauds
Nicar/clev rx HTN urgency
Nimo rx subarachnoid hemorrhage
Veramipil & dialtizem
Ca channel blockers that rx angina HTN, & Afib
Classification: sympathomimetics – direct –– selective 1 agonist
Mechanism of Action: stimulates β1- adrenergic receptors with minor effect on HR or peripheral blood vessels –– increases CO without significantly increasing HR
Clinical Indications: heart failure, cardiogenic shock (inotropic), cardiac stress testing
Adverse Effects: hypertension, tachycardia, PVCs, arrhythmias
Dobutamine β1 >β 2, 𝛂
Classification: PDE-5 inhibitor
Mechanism of Action: inhibits PDE-5 leading to increased cGMP resulting in prolonged vasodilatory effect of NO –– pulmonary artery relaxation
Clinical Indications: pulmonary hypertension, erectile dysfunction
Adverse Effects: headache, flushing, insomnia, transient blue-green tinting of vision (related to inhibition of retinal PDE6 that is involved in transduction)
Sildenafil
Classification: antiarrhythmics – sodium channel blocker (class IA)
Mechanism of Action: moderate Na+ channel blockade – increases AP duration, increases effective refractory period in ventricular action potential, increases QT interval, some potassium channel blocking effects –– metabolized via N-acetyltransferase
Clinical Indications: both atrial and ventricular arrhythmias, especially re-entrant and ectopic SVT and VT (WPW, Afib, V Tach)
Adverse Effects: reversible SLE-like syndrome, thrombocytopenia, torsades de pointes due to increased QT interval
Procainamide
Very low LDL
high HDL
Low TG
Inhibit HMG-CoA
Avoid with fibrates
Statins
Very low LDL
Very high HDL
Low TG
Inhibit lipolysis (vitamin btw)
Niacin
Low LDL
High HDL
Very very low TG
+ve PARR alpha
avoid with statins
Fibrates
Classification: β2 agonist (short acting)
Mechanism of Action: relaxes bronchial smooth muscle –– bronchodilation
Clinical Indications: acute exacerbations and prophylaxis of exercise-induced
Adverse Effects: tremor, arrythmia, tolerance, tachyphylaxis
Albuterol
Classification: β2 agonist (short acting)
Mechanism of Action: relaxes bronchial smooth muscle –– bronchodilation
Clinical Indications: asthma prophylaxis
Adverse Effects: tremor, arrythmia, tolerance, tachyphylaxis
Salbutamol
Rx hyperkalemia
Insulin + glucose, calcium gluconate, β2 agonists
Classification: antileukotriene
Mechanism of Action: 5-lipoxygenase pathway inhibitor – blocks conversion of arachidonic acid to leukotrienes –– LTB4 (chemotactic) LTC4/ LTD4 (bronchoconstriction) –– short acting
Clinical Indications: asthma prophylaxis
Adverse Effects: hepatotoxic
Zileuton
Classification: antileukotriene
Mechanism of Action: antagonists at LTD4 receptors –– block leukotriene receptors (CysLT1): competitive antagonist –– reduce bronchoconstriction in asthma –– additive action with 2-adrenoreceptor agonist
Clinical Indications: prophylaxis –– especially good for aspirin-induced and exercise-induced asthma –– mainly used as add-on therapy to inhaled corticosteroids and long-acting 2 agonist –– safe during pregnancy
Adverse Effects: hepatotoxic
Montelukast
HTN only
AE
Orthostatic hypotension
Prazosin
BPH & HTN
AE: Ortho hypo
Doxazosin & Terazosin
Just BPH
AE: Floppy iris
Tamsulosin
Rx pheochromocytoma
Phenoxybenzamine (irr a antagonist to avoid HTN crisis)
Classification: selective 1a/d blockers
Mechanism of Action: inhibit 1 receptor leading to relaxation of smooth muscle (bladder neck, prostate) resulting in decreased urinary obstruction
Adverse Effects: ‘first dose’ hypotension and syncope, headache
Treatment for BPH
Tamsulosin
Classification: sympathomimetics – indirect
Mechanism of Action: blocks NE reuptake and dopamine reuptake –– also blocks Na+/K-ATPase
Clinical Indications: causes vasoconstriction and local anesthesia – caution when giving beta-blockers if cocaine intoxication is suspected – can lead to unopposed ɑ1 activation)
Adverse Effects: highly addictive, hypertension, arrythmias, seizures
Cocain
Classification: cholinomimetic agents – direct agonist
Mechanism of Action: muscarinic agonist activated M3 receptor (increases IP3 and DAG) leading to contraction of detrusor smooth muscle resulting in increased bladder emptying– resistant to AChE, no nicotinic activity
Clinical Indications: urinary retention, ileus (postop/neurogenic)
Adverse Effects: parasympathomimetic effects, cyclospasm, diarrhea, urinary urgency, vasodilation, reflex tachycardia, sweating
Bethanechol: Bladder
Classification: direct-acting muscarinic agonist (M1 and M3)
Mechanism of Action: bind and activate muscarinic receptors – M1 receptors are common in secretory glands and their activation results in increased secretion from the secretory glands –– M3 receptors are found in smooth muscles and glands and their activation results in smooth muscle contraction and increased glandular secretion
Clinical Indications: xerostomia (Sjörgen Syndrome)
Adverse Effects: sweating, nausea, rhinitis, sinusitis, URIs
Cevimeline
Mechanism of Action: chemical antagonist of organophosphates –– regenerates AChE via dephosphorylation if given early – reactivate cholinesterase inactivated by phosphating due to OP (mainly outside CNS)
Clinical Indications: organophosphate poisoning –– works on nicotinic effects
Adverse Effects: muscle weakness
Pralidoxime (quaternary amine) (-oxime)
Classification: sympatholytic – ɑ2 agonist presynaptic
Mechanism of Action: stimulate prejunctional receptors in the CNS to decrease sympathetic outflow, decrease TPR and HR
Clinical Indications: hypertensive urgency, ADHD, Tourette syndrome, symptom control in opioid withdrawal
Adverse Effects: CNS depression, bradycardia, hypotension, respiratory depression, miosis, rebound hypertension with abrupt cessation
Clonidine
Classification: muscarinic antagonist (competitive at all M receptors)
Mechanism of Action: produce mydriasis and cycloplegia –– bronchodilation and decrease airway secretions –– decrease stomach acid secretion –– decrease GI motility –– decrease bladder urgency in cystitis
Clinical Indications: bradycardia and for ophthalmic applications (long action), antispasmodic, antisecretory, management of AChE inhibitor overdose, antidiarrheal
Adverse Effects: increased body temperature (decrease sweating), tachycardia, dry mouth, dry, flushed skin, cycloplegia, constipation, disorientation –– can cause acute-angle glaucoma in elderly, urinary retention in men with prostatic hyperplasia and hyperthermia in infants
Atropine
Classification: cholinomimetic agent – indirect agonist (anticholinesterase)
Mechanism of Action: inhibits cholinesterase and amplifies endogenously released Ach –– increase Ach – freely crosses blood brain barrier into CNS
Clinical Indications: glaucoma, antidote for anticholinergic toxicity (atropine)
Adverse Effects: increased parasympathetic effects (especially N/V/D, urinary urgency), seizures
Physostigmine (tertiary amine)
Classification: cholinomimetic agent – indirect agonist (anticholinesterase)
Mechanism of Action: increase ACh
Clinical Indications: first line for Alzheimer disease
Adverse Effects: nausea and vomiting
Donepezil (also Rivastigmine, galantamine
Classification: antiarrhythmics –– beta-blocker (class II) –– β1 selective
Mechanism of Action: decrease SA and AV nodal activity by decreasing cAMP, decreasing Ca2+ currents –– suppress abnormal pacemakers by decreasing slope of phase 4 –– AV node particularly sensitive (increase PR interval)
Clinical Indications: SVT, ventricular rate control for atrial fibrillation/ atrial flutter
Adverse Effects: impotence, exacerbation of COPD and asthma, cardiovascular effects (bradycardia, AV block, HF), CNS effects (sedation, sleep alterations) – may mask hypoglycemia
Atenolol
Classification: beta-blocker
Mechanism of Action: blocks action of NE at ciliary epithelium –– decrease aqueous humor synthesis via Beta 2
Adverse Effects: no pupillary or vision changes
Timolol
Classification: prostaglandin (PGF2) analog (-toprost)
Mechanism of Action: increase outflow of aqueous humor via decrease resistance of flow through uveoscleral pathway
Adverse Effects: darkens color of iris (browning), eyelash growth, macular edema in aphasics (have no eye lens), reactivation of uveitis
Latanoprost
Classification: cholinomimetic agent: direct agonist
MOA: act like Ach
Indications:
contracts ciliary muscle of the eye: open angle glaucoma
pupillary sphincter: closed angle glaucoma
xerostomia: SJS (increases tear, sweat, saliva production)
A/E: exacerbation of COPD, asthma, peptic ulcer
Pilocarpine
Glaucoma B-blockers & their effects?
Timolol, Betaxolol & Carteolol
Reduce aqueous humor synthesis no pupil or vision changes
Glaucoma Alpha agonists & their effects?
apraclonidine & Brimonidine
Reduces aqueous humor synthesis & increase uveoscleral out flow
Causes mydriases so avoid in closed angle glaucoma
Glaucoma Diuretic & effects?
Acetazolamide (carbonic anhydrase inhibitor PCT)
Reduced aqueous humor production no pupil or vision changes
Glaucoma Prostaglandins & effects?
Latanoprost & Bimatoprost
Increase uveoscleral outflow
Darken iris & eyelash growth
Glaucoma M3 agonists & effects?
Pilocarpine & carbachol (direct) miosis & cyclopsams Increases outflow through trabecular meshwork used in acute angle/closed glaucoma
Physostigmine- (indirect
Diphenhydramine, dimenhydrinate. chlorpheniramine & doxylamine
H1 antihistamines for allergies & motion sickness
AE: Sedation
Loratidine, Fexofenadine, desloratadine, & cetirizine
H2 Antihistamines just for allergies no AE cause they don’t breach CNS
