Receptors simplified & all drugs for B2 (BBH's notes) Flashcards
Describe the following for 2nd generation H1 blockers (antihistamines):
What drugs do they include?
What are their clinical uses?
What are the adverse effects?
Drugs:
LoratADINE
FexofenADINE
DesloratADINE
Cetirizine
Clinical use:
1) Allergic rhinitis
Adverse effects:
Fewer side effects because it doesn’t enter the CNS
Drugs:
LoratADINE
FexofenADINE
DesloratADINE
Cetirizine
Clinical use:
1) Allergic rhinitis
Adverse effects:
Fewer side effects because it doesn’t enter the CNS
Describes which type of drug?
2nd generation H1 Blockers (antihistamines)
Describe the following for Misoprostol:
What is the drug type?
What is the MOA?
What are the clinical uses?
What are the adverse effects?
Drug type:
PGE1 analog
MOA:
It increases the production & secretion of gastric mucus while reducing the production of gastric acid
Clinical use:
1) Prevent NSAID-induced peptic ulcers (protective)
2) An off-label labor inducer (ripens the cervix)
Adverse effects:
1) Nausea/vomiting/diarrhea
2) May cause abortion
3) Vaginal bleeding
4) Uterine cramping
5) Flushing
6) Tachycardia
Drug type:
PGE1 analog
MOA:
It increases the production & secretion of gastric mucus while reducing the production of gastric acid
Clinical use:
1) Prevent NSAID-induced peptic ulcers (protective)
2) An off-label labor inducer (ripens the cervix)
Adverse effects:
1) Nausea/vomiting/diarrhea
2) May cause abortion
3) Vaginal bleeding
4) Uterine cramping
5) Flushing
6) Tachycardia
Describes which drug?
Misoprostol:
Describe the following for Alprostadil:
What is the drug type?
What is the MOA?
What are the clinical uses?
What are the adverse effects?
Drug type:
PGE1 analog
MOA:
It relaxes smooth muscle in the ductus arteriosus
Clinical uses:
1) Keep the PDA open
2) Impotence
Adverse effects:
1) Hypotension
2) Nausea/vomiting/diarrhea
3) Vaginal bleeding
4) Flushing
5) Tachycardia
Drug type:
PGE1 analog
MOA:
It relaxes smooth muscle in the ductus arteriosus
Clinical uses:
1) Keep the PDA open
2) Impotence
Adverse effects:
1) Hypotension
2) Nausea/vomiting/diarrhea
3) Vaginal bleeding
4) Flushing
5) Tachycardia
Describes which drug?
Alprostadil:
Describe the following for 1st generation H1 blockers (antihistamines):
What are the drugs?
What is the MOA?
What are the clinical uses?
What are the adverse effects?
Diphenhydramine
Dimenhydrinate
Doxylamine
Chlorpheniramine
Clinical uses:
1) Allergies
2) Motion sickness
3) Vomiting in pregnancy
4) Sleep aid
Adverse effects:
1) Sedation
2) Antimuscarinic effects
3) Anti a adrenergic effects
Diphenhydramine
Dimenhydrinate
Doxylamine
Chlorpheniramine
Clinical uses:
1) Allergies
2) Motion sickness
3) Vomiting in pregnancy
4) Sleep aid
Adverse effects:
1) Sedation
2) Antimuscarinic effects
3) Anti a adrenergic effects
Describes which kind of drugs?
1st generation H1 blockers (antihistamines):
“all it takes is 1 daffodile or dog to cause drowsiness & Congestion”
Describe the following for acetaminophen:
What is the drug type?
What is the MOA?
What are the clinical uses?
What are the adverse effects?
Drug type:
NSAID
MOA:
It reversibly inhibits cyclooxygenase in the CNS (mostly) & it’s activated peripherally meaning it’s not great as an anti-inflammatory
Clinic uses:
1) Antipyretic
2) Analgesic (acts on the cannabinoid receptors)
Adverse effects:
1) Hepatic necrosis (OD)
Drug type:
NSAID
MOA:
It reversibly inhibits cyclooxygenase in the CNS (mostly) & it’s activated peripherally meaning it’s not great as an anti-inflammatory
Clinic uses:
1) Antipyretic
2) Analgesic (acts on the cannabinoid receptors)
Adverse effects:
1) Hepatic necrosis (OD)
Describes which drug?
Acetaminophen
Describe the following for indomethacin:
What is the drug type?
What is the MOA?
What are the clinical uses?
What are the adverse effects?
Drug type:
NSAID
MOA:
It reversibly inhibits COX1 & COX2 to block prostaglandin synthesis (pro-inflammatory)
Clinical uses:
1) Antipyretic
2) Analgesic
3) Anti-inflammatory
4) Close a PDA
Adverse effects:
1) Interstitial nephritis
2) Gastric ulcers
3) Renal ischemia
4) Aplastic anemia
Drug type:
NSAID
MOA:
It reversibly inhibits COX1 & COX2 to block prostaglandin synthesis (pro-inflammatory)
Clinical uses:
1) Antipyretic
2) Analgesic
3) Anti-inflammatory
4) Close a PDA
Adverse effects:
1) Interstitial nephritis
2) Gastric ulcers
3) Renal ischemia
4) Aplastic anemia
Describes which drug?
Indomethicin
Indomethacin
Acetaminophen
Are examples of which type of drug?
NSAIDS
Describe the following for Colchicine:
What is the drug type?
What is the MOA?
What are the clinical uses?
What are the adverse effects?
Drug type:
Acute gout drug
MOA:
It binds & stabilizes tubulin to inhibit microtubule polymerization resulting in impaired neutrophil chemotaxis & degranulation causing decreased leukotriene (LTB4), leukocyte, & granulocyte migration
Clinical uses:
1) Acute gout & gout prophylaxis
Adverse effects:
1) Diarrhea
2) Acute Gi pain
3) Hematuria
4) Myelosuppression
5) Gastritis
6) Peripheral neuropathy (with long-term use)
Drug type:
Acute gout drug
MOA:
It binds & stabilizes tubulin to inhibit microtubule polymerization resulting in impaired neutrophil chemotaxis & degranulation causing decreased leukotriene (LTB4), leukocyte, & granulocyte migration
Clinical uses:
1) Acute gout & gout prophylaxis
Adverse effects:
1) Diarrhea
2) Acute Gi pain
3) Hematuria
4) Myelosuppression
5) Gastritis
6) Peripheral neuropathy (with long-term use)
Describes which drug?
Colchicine
Describe the following for Sulfinpyrazone:
What is the drug type?
What is the MOA?
What are the clinical uses?
What are the adverse effects?
Drug type:
Chronic anti-gout
MOA:
It inhibits renal reabsorption of uric acid AVOID in acute gout cases (it’ll make it worse!)
Clinical uses:
1) Chronic gout
Adverse effects:
1) Precipitate uric acid calculi (kidney stones)
2) Nephrotic syndrome
3) Aplastic anemia
4) Allergy
Drug type:
Chronic anti-gout
MOA:
It inhibits renal reabsorption of uric acid AVOID in acute gout cases (it’ll make it worse!)
Clinical uses:
1) Chronic gout
Adverse effects:
1) Precipitate uric acid calculi (kidney stones)
2) Nephrotic syndrome
3) Aplastic anemia
4) Allergy
Describes which drug?
Sulfinpyrazone
Describe the following for Probenecid:
What is the drug type?
What is the MOA?
What are the clinical uses?
What are the adverse effects?
Drug type:
Chronic gout drug
MOA:
It inhibits the reabsorption of uric acid in the PCT & it inhibits penicillin secretion from the DCT (promotes retention) AVOID in acute gout (it will get worse!)
Clinical uses:
1) Chronic gout
2) Prophylaxis of chronic gout
Adverse effects:
1) Precipitate uric acid calculi (kidney stones)
2) Nephrotic syndrome
3) Aplastic anemia
4) Allergy
Drug type:
Chronic gout drug
MOA:
It inhibits the reabsorption of uric acid in the PCT & it inhibits penicillin secretion from the DCT (promotes retention) AVOID in acute gout (it will get worse!)
Clinical uses:
1) Chronic gout
2) Prophylaxis of chronic gout
Adverse effects:
1) Precipitate uric acid calculi (kidney stones)
2) Nephrotic syndrome
3) Aplastic anemia
4) Allergy
Describes which drug?
Probenecid
Describe the following for Ergotamine:
What is the drug type?
What is the MOA?
What are the clinical uses?
What are the adverse effects?
Drug type:
An ergot alkaloid
MOA:
It acts as a partial agonist at 5-HT2 (serotonin) receptors in the vasculature & maybe the CNS resulting in vasoconstriction & reduced pulsation in the cerebral vessels
Clinical uses:
1) Acute migraine attacks
Adverse effects:
1) Gi distress
2) Ischemia/gangrene (if vasoconstriction is prolonged)
3) Abortion near term (avoid in preggos)
Drug type:
An ergot alkaloid
MOA:
It acts as a partial agonist at 5-HT2 (serotonin) receptors in the vasculature & maybe the CNS resulting in vasoconstriction & reduced pulsation in the cerebral vessels
Clinical uses:
1) Acute migraine attacks
Adverse effects:
1) Gi distress
2) Ischemia/gangrene (if vasoconstriction is prolonged)
3) Abortion near term (avoid in preggos)
Describes which drug?
Ergotamine
Describe the following for Sumatriptan:
What is the drug type?
What is the MOA?
What are the clinical uses?
What are the adverse effects?
Drug type:
A triptan aka serotonin agonist
MOA: An agonist at 5-HT(B1/D1) to inhibit the trigeminal nerve affects via vasoactive peptide release to induce vasoconstriction
Clinical uses:
1) Acute migraine
2) Cluster headache attacks
Adverse effects:
1) Coronary vasospasms (AVOID in CAD or vasospastic angina)
2) Mild paresthesia
3) Serotonin syndrome
Drug type:
A triptan aka serotonin agonist
MOA: An agonist at 5-HT(B1/D1) to inhibit the trigeminal nerve affects via vasoactive peptide release to induce vasoconstriction
Clinical uses:
1) Acute migraine
2) Cluster headache attacks
Adverse effects:
1) Coronary vasospasms (AVOID in CAD or vasospastic angina)
2) Mild paresthesia
3) Serotonin syndrome
Describes which drug?
Sumatriptan
Sumatriptan
Ergotamine
Are both used to treat which conditions
Migraines (both)
Cluster headache attacks (S)
Describe the following for warfarin toxicity:
What are the symptoms?
What are the treatments/antidotes?
Signs:
1) Bleeding
2) Skin necrosis (if there’s low protein C)
Rx:
Fresh frozen plasma (acutely)
Vitamin K (not acutely)
Signs:
1) Bleeding
2) Skin necrosis (if there’s low protein C)
Rx:
Fresh frozen plasma (acutely)
Vitamin K (not acutely)
Indicate which type of toxicity?
Warfarin toxicity
Describe the following for Heparin toxicity:
What are the symptoms?
What are the treatments/antidotes?
Signs:
1) Bleeding
Rx:
Protamine sulfate (it’s a +ve charged molecule that binds -ve charged heparin)
Signs:
1) Bleeding
Rx:
Protamine sulfate
Describes which type of toxicity?
Heparin toxicity
Describe the following for digoxin toxicity:
What are the symptoms?
What are predisposing factors/risks?
- factors associated with a poor prognosis
What are the treatments/antidotes?
Signs:
1) Cholinergic effects (nausea, vomiting, diarrhea)
2) blurry yellow vision
3) Arrythmias
4) AV block
Risks:
1) Renal failure
2) Hypokalemia (ass with poor prognosis)
3) Drugs that displace digoxin from its tissue binding sites (i.e verapamil, amiodarone, quinidine)
Poor prog:
- Hypokalemia
- Hypomagnesemia
- Hypercalcemic
Rx:
1) anti-digoxin Fab fragments ***
2) Slowly normalize K+
3) Antiarrhythmic drugs
4) Cardiac pacer (in severe cases)
5) Mg2+ supplement
6) Block the vagus nerve (propranolol or atropine)
Signs:
1) Cholinergic effects (nausea, vomiting, diarrhea)
2) blurry yellow vision
3) Arrythmias
4) AV block
Risks:
1) Renal failure
2) Hypokalemia (ass with poor prognosis)
3) Drugs that displace digoxin from its tissue binding sites (i.e verapamil, amiodarone, quinidine)
Poor prog:
- Hypokalemia
- Hypomagnesemia
- Hypercalcemic
Rx:
1) anti-digoxin Fab fragments ***
2) Slowly normalize K+
3) Antiarrhythmic drugs
4) Cardiac pacer (in severe cases)
5) Mg2+ supplement
6) Block the vagus nerve (propranolol or atropine)
Describes which type of toxicity?
Digoxin toxicity
Describe the following for Aspirin/Salicylate poisoning:
What happens?
What are the symptoms?
What are predisposing factors/risks?
- factors associated with a poor prognosis
What are the treatments/antidotes?
Patho:
Toxic doses cause respiratory alkalosis early on that then turns into a mixed metabolic acidosis/respiratory alkalosis later on
Signs:
1) Confusion/Stupor
2) Lethargy
3) Ataxia
4) Nystagmus
5) Hypothermia
6) Respiratory failure
7) Coma/death
Rx:
1) NaHCHO3 (bicarbonate to alkalize the urine)
2) Dialysis
3) Electrolytes
Patho:
Toxic doses cause respiratory alkalosis early on that then turns into a mixed metabolic acidosis/respiratory alkalosis later on
Signs:
1) Confusion/Stupor
2) Lethargy
3) Ataxia
4) Nystagmus
5) Hypothermia
6) Respiratory failure
7) Coma/death
Rx:
1) NaHCHO3 (bicarbonate to alkalize the urine)
2) Dialysis
3) Electrolytes
Describes which type of toxicity/poisoning?
Aspirin/Salicylate poisoning
Describe the following for Atropine poisoning:
What are the symptoms?
What are the treatments/antidotes?
Aka Belladona or deadly nightshade berries
Signs:
1) Tachycardia
2) Hypertension
3) Hyperthermia
4) Delirium
5) Mydriasis
Rx:
1) Physostigmine (an indirect M agonist to inhibit AChE & increase the available Ach to control the symptoms)
Aka Belladona or deadly nightshade berries
Signs:
1) Tachycardia
2) Hypertension
3) Hyperthermia
4) Delirium
5) Mydriasis
Rx:
1) Physostigmine (an indirect M agonist to inhibit AChE & increase the available Ach to control the symptoms)
Describes which type of poisoning?
Atropine poisoning
Describe the following for iron poisoning:
What are the symptoms?
What are the complications?
What are the treatments/antidotes?
Sigs:
1) Severe Gi distress
2) Dyspnea
3) Shock
4) Coma
Comps:
Necrotizing gastroenteritis
Hematemesis & bloody diarrhea
Rx:
1) Deferoxamine, Deferasirox, & Deferiprone (iron chelators)
2) Gastric aspiration
3) Carbonate lavage
Sigs:
1) Severe Gi distress
2) Dyspnea
3) Shock
4) Coma
Comps:
Necrotizing gastroenteritis
Hematemesis & bloody diarrhea
Rx:
1) Deferoxamine, Deferasirox, & Deferiprone (iron chelators)
2) Gastric aspiration
3) Carbonate lavage
Describes which type of poisoning?
Iron poisoning
Describe the following for Acetaminophen poisoning:
What happens?
What are the symptoms?
What are the complications?
What are the treatments/antidotes?
Patho:
Acetaminophens metabolite (NAPQI) depletes all the glutathione & it forms toxic tissue byproducts in the liver (hepatic necrosis)
Signs:
1) Hepatic & renal failure
2) Mild anorexia
3) Delayed jaundice
4) Nausea/vomiting
Rx:
1) N-acetylcysteine (to replenish the glutathione to break down acetaminophens byproduct)
Patho:
metabolite (NAPQI) depletes all the glutathione & it forms toxic tissue byproducts in the liver (hepatic necrosis)
Signs:
1) Hepatic & renal failure
2) Mild anorexia
3) Delayed jaundice
4) Nausea/vomiting
Rx:
1) N-acetylcysteine (to replenish the glutathione)
Acetaminophen poisoning
Describe the following for Organophosphate poisoning:
What predisposes/risks?
What happens?
What are the symptoms?
What are the complications?
What are the treatments/antidotes?
Risk:
Insecticides (usually farmers)
Patho:
The organophosphates irreversibly bind AChE which can then only be freed by dephosphorylation from atropine or pralidoxime
Signs:
Muscarinic (DUMBBELLSS)
1) Diarrhea (colic)
2) Urination
3) Miosis
4) Bronchospasms (constriction)
5) Bradycardia
6) Emesis
7) Lacrimation
8) Sweating/Salivation
Nicotinic (CNS effects)
1) Seizures
2) Lethargy
3) Coma
4) Respiratory/CNS depression
Rx:
Atropine (antagonizes M receptors)
Pralidoxime (dephosphorylation to regen AChE if given early)
Risk:
Insecticides (usually farmers)
Patho:
irreversibly bound AChE which can then only be freed by dephosphorylation from atropine or pralidoxime
Signs:
Muscarinic (DUMBBELLSS)
1) Diarrhea (colic)
2) Urination
3) Miosis
4) Bronchospasms (constriction)
5) Bradycardia
6) Emesis
7) Lacrimation
8) Sweating/Salivation
Nicotinic (CNS effects)
1) Seizures
2) Lethargy
3) Coma
4) Respiratory/CNS depression
Rx:
Atropine (antagonizes M receptors)
Pralidoxime (dephosphorylation to regen AChE if given early)
Describes which type of poisoning?
Organophosphate poisoning
Describe the following for
Clopidogrel
Prasugrel
Ticagrelor
Ticlopidine:
What is the drug type?
What is the MOA?
What are the clinical uses?
What are the adverse effects?
Drug type:
ADP receptor antagonists
MOA:
They reduce ADP-induced expression of GpIIb/IIa
Clinical uses:
1) Aspirin-like effects (anti-inflammatory)
2) Antiplatelet treatment
Adverse effects:
1) Neutropenia (ticlopidine)
2) Thrombotic thrombocytopenic purpura (TTP)
Drug type:
ADP receptor antagonists
MOA:
They reduce ADP-induced expression of GpIIb/IIa
Clinical uses:
1) Aspirin-like effects (anti-inflammatory)
2) Antiplatelet treatment
Adverse effects:
1) Neutropenia
2) Thrombotic thrombocytopenic purpura (TTP)
Describes which drugs?
Clopidogrel
Prasugrel
Ticagrelor
Ticlopidine
Describe the following for Heparin:
What is the drug type?
What is the MOA?
What are the clinical uses?
What are the adverse effects?
Avoid use in which conditions?
Durg type:
An antithrombin 3 activator
MOA:
It activates antithrombin 3 to reduce the action of thrombin (IIa) & factors resulting in a conformational change in antithrombin that makes reactive sites more accessible to proteases
Clinical uses:
1) Immediate anticoagulation for pulmonary embolism
2) Acute coronary syndrome
3) MI
4) DVT (safe in preggos)
Adverse effects:
1) Bleeding
2) Thrombocytopenia/thrombosis
3) Osteoporosis
4) Drug-drug interactions (warfarin)
5) Hyperkalemia
AVOID:
1) Hypersensitivities
2) Active bleeding
3) Active TB inf
4) Significant thrombocytopenia
5) Advanced hepatic/renal disease
6) Hemophilia
7) GIT ulcers
8) Infective endocarditis
Durg type:
An antithrombin 3 activator
MOA:
It activates antithrombin 3 to reduce the action of thrombin (IIa) & factors resulting in a conformational change in antithrombin that makes reactive sites more accessible to proteases
Clinical uses:
1) Immediate anticoagulation for pulmonary embolism
2) Acute coronary syndrome
3) MI
4) DVT (safe in preggos)
Adverse effects:
1) Bleeding
2) Thrombocytopenia/thrombosis
3) Osteoporosis
4) Drug-drug interactions (warfarin)
5) Hyperkalemia
AVOID:
1) Hypersensitivities
2) Active bleeding
3) Active TB inf
4) Significant thrombocytopenia
5) Advanced hepatic/renal disease
6) Hemophilia
7) GIT ulcers
8) Infective endocarditis
Describes which drug?
Heparin
Describe the following for Enoxaparin:
What is the drug type?
What is the MOA?
What are the clinical uses?
What are the adverse effects?
Avoid use in which conditions?
Drug type:
Low molecular weight heparin
MOA:
It binds to antithrombin 3 to reduce thrombin similar to heparin but it has a much longer 1/2 life & it doesn’t need to be monitored as much because it’s more predictable & has less risk of adverse effects
Clinical uses:
1) Anticoagulant
Adverse effects:
1) Bleeding
2) Thrombocytopenia/thrombosis (Less risk)
3) Osteoporosis
4) Drug-drug interactions
5) Hyperkalemia
AVOID:
not for patients with renal failure
Drug type:
Low molecular weight heparin
MOA:
It binds to antithrombin 3 to reduce thrombin similar to heparin but it has a much longer 1/2 life & it doesn’t need to be monitored as much because it’s more predictable & has less risk of adverse effects
Clinical uses:
1) Anticoagulant
Adverse effects:
1) Bleeding
2) Thrombocytopenia/thrombosis (Less risk)
3) Osteoporosis
4) Drug-drug interactions
5) Hyperkalemia
AVOID:
not for patients with renal failure
Describes which drug?
Enoxaparin
Which drugs are mainly used for asthma?
Zileuton & Montelukast
Zileuton & Montelukast
Are drugs often used to treat which condition?
bronchial asthma
Describe the following for Zileuton:
What is the drug type?
What is the MOA?
What is the clinical use?
What is an adverse effect?
Drug type:
An antileukotriene
MOA:
It inhibits the 5-lipoxygenase pathway to block the conversion of arachnoid acid into leukotrienes reducing the levels of leukotrienes (LTB4 (chemotactic) & LTC4/D4 (bronchoconstriction))
Clinical use:
1) Prophylaxis of asthma
Adverse effects:
1) Hepatotoxicity
Drug type:
An antileukotriene
MOA:
It inhibits the 5-lipoxygenase pathway to block the conversion of arachnoid acid into leukotrienes reducing the levels of leukotrienes (LTB4 (chemotactic) & LTC4/D4 (bronchoconstriction))
Clinical use:
1) Prophylaxis of asthma
Adverse effects:
1) Hepatotoxicity
Describes which drug?
Zileuton
Describe the following for Montelukast:
What is the drug type?
What is the MOA?
What is the clinical use?
What is an adverse effect?
Drug type:
An antileukotriene
MOA:
An antagonist at leukotriene receptors (LTD4/C4 involved in bronchoconstriction), it’s safe to use in preggos
Clinical uses:
1) Prophylaxis for aspirin or exercise induced asthma (added with an inhaled corticosteroid & B2 blocker)
Adverse effects:
1) hepatotoxicity
Drug type:
An antileukotriene
MOA:
An antagonist at leukotriene receptors (LTD4/C4 involved in bronchoconstriction), it’s safe to use in preggos
Clinical uses:
1) Prophylaxis for aspirin or exercise induced asthma (added with an inhaled corticosteroid & B2 blocker)
Adverse effects:
1) hepatotoxicity
Describes which drug?
Montelukast
Describe the following for Pralidoxime:
What is the drug type?
What is the MOA?
What is the clinical use?
What is an adverse effect?
Drug type:
A quaternary amine & chemical antagonist of organophosphates
MOA:
It regenerates AChE by dephosphorylation if given early enough
Clinical use:
1) Organophosphate poisoning
Adverse effect:
1) Muscle weakness
Drug type:
A quaternary amine & chemical antagonist of organophosphates
MOA:
It regenerates AChE by dephosphorylation if given early enough
Clinical use:
1) Organophosphate poisoning
Adverse effect:
1) Muscle weakness
Describes which drug?
Pralidoxime
Describe the following for Epoetin alfa (Erythropoietin):
What drug type?
What is the MOA?
What are the clinical uses?
What are the adverse effects?
Drug type:
An erythropoiesis-stimulating agent
MOA:
It is an erythropoietin receptor agonist that is expressed on RBC progenitors
Clinical uses:
1) Anemias (from chronic renal failure, HIV, cancer, or premature birth)
2) Prevent anemias during transfusions
Adverse effects:
1) Hypertension
2) Thrombotic complications
3) Pure RBC aplasia
Drug type:
An erythropoiesis-stimulating agent
MOA:
It is an erythropoietin receptor agonist that is expressed on RBC progenitors
Clinical uses:
1) Anemias (from chronic renal failure, HIV, cancer, or premature birth)
2) Prevent anemias during transfusions
Adverse effects:
1) Hypertension
2) Thrombotic complications
3) Pure RBC aplasia
Describes which drug?
Epoetin alfa (erythropoietin)
Describe the following for Thiazide diuretics:
What are the drugs included?
What is the MOA?
- effects
What are the clinical uses?
What are the adverse effects?
Drugs:
Hydrochlorothiazide
Chlorthalidone
Metolazone
MOA:
They inhibit NaCl resorption in the early DCT resulting in reduced diluting capacity of the nephron causing more Ca2+ retention
Effects:
1) Na/Cl-/K+ excretion
2) Ca2+ retention
3) Alkalemia (HCO3) retention
Clinical uses:
1) Hypertension
2) Heart failure
3) Idiopathic hypercalcemia
4) Nephrogenic diabetes insipidus
5) Osteoporosis
Adverse effects:
1) Hypokalemic metabolic alkalosis
2) Hyponatremia
3) Hyperglycemia
4) Hyperuricemia
5) Hypercalcemia
6) Sulfa allergy
7) Hyperlipidemia
Drugs:
Hydrochlorothiazide
Chlorthalidone
Metolazone
MOA:
They inhibit NaCl resorption in the early DCT resulting in reduced diluting capacity of the nephron causing more Ca2+ retention
Effects:
1) Na/Cl-/K+ excretion
2) Ca2+ retention
3) Alkalemia (HCO3) retention
Clinical uses:
1) Hypertension
2) Heart failure
3) Idiopathic hypercalcemia
4) Nephrogenic diabetes insipidus
5) Osteoporosis
Adverse effects:
1) Hypokalemic metabolic alkalosis
2) Hyponatremia
3) Hyperglycemia
4) Hyperuricemia
5) Hypercalcemia
6) Sulfa allergy
7) Hyperlipidemia
Describes which group of diuretics
Thiazide diuretics
Hydrochlorothiazide
Chlorthalidone
Metolazone
Are examples of which type of diuretics that act on which part of the nephron?
Thiazide diuretics that act on the early DCT
Thiazide diuretics that act on the early DCT include which drugs?
Hydrochlorothiazide
Chlorthalidone
Metolazone
Describe the following for Loop diuretics:
What are the drugs?
What is the MOA?
-effects
What are the clinical uses?
What are the adverse effects?
Drugs:
Furosemide
Bumetanide
Torsemide
MOA:
These are sulfonamide loop diuretics that act on the thick ascending loop of Henle to inhibit Na+, K+, & Cl- co-transporters resulting in:
Effects:
1) Ca2+/K+/NaCl excretion
2) Alkalemia (HCO3) retention
3) Abolished hypertonicity of the medulla
4) Elevated PGE (vasodilation of afferent arteriole
Clinical uses:
1) Edematous states (HF, Cirrhosis, Nephrotic syndrome, Pulmonary edema)
2) Hypertension
3) Hypercalcemia/kalemia/natremia
Adverse effects:
1) Ototoxicity
2) Hypokalemia
3) Hypomagnesemia
4) Dehydration
5) Allergy (Sulfa)
6) Alkalosis (metabolic)
7) Nephritis
8) Gout
“OHH DAANG!”
Drugs:
Furosemide
Bumetanide
Torsemide
MOA:
These are sulfonamide loop diuretics that act on the thick ascending loop of Henle to inhibit Na+, K+, & Cl- co-transporters resulting in:
Effects:
1) Ca2+/K+/NaCl excretion
2) Alkalemia (HCO3) retention
3) Abolished hypertonicity of the medulla
4) Elevated PGE (vasodilation of afferent arteriole
Clinical uses:
1) Edematous states (HF, Cirrhosis, Nephrotic syndrome, Pulmonary edema)
2) Hypertension
3) Hypercalcemia/kalemia/natremia
Adverse effects:
1) Ototoxicity
2) Hypokalemia
3) Hypomagnesemia
4) Dehydration
5) Allergy (Sulfa)
6) Alkalosis (metabolic)
7) Nephritis
8) Gout
“OHH DAANG!”
Describes which drug type?
Loop diuretics
Drugs:
Furosemide
Bumetanide
Torsemide
Are examples of which type of diuretics that act on what part of the nephron?
Loop diuretics that act on the thick ascending limb of the loop of Henle
Loop diuretics that act on the thick ascending limb of the loop of Henle, include which drugs?
Furosemide
Bumetanide
Torsemide
Describe the following for potassium sparring diuretics:
What are the drugs?
What is the MOA?
What are the effects?
What are the clinical uses?
What are the adverse side effects?
Drugs:
Spironolactone
Eplerenone
Amiloride
Triamterene
MOA:
1) Spironolactone & Eplerenone (are competitive antagonists in the cortical collecting tubule
2) Amiloride & Triamterene (are Na channel blockers in the cortical collecting tubule)
Effects:
1) Acidemia (K+ & H+ retention)
2) NaCl excretion
Clinical uses:
1) Hyperaldosteronism
2) Hypokalemia
3) Heart failure
4) Nephrogenic Diabetes Insipidus
5) Anti-Androgenics
Adverse effects:
1) Hyperkalemia & arrythmia
2) Endocrine symptoms (Gynecomastia)
3) Metabolic acidosis
Drugs:
Spironolactone
Eplerenone
Amiloride
Triamterene
MOA:
1) Spironolactone & Eplerenone (are competitive antagonists in the cortical collecting tubule
2) Amiloride & Triamterene (are Na channel blockers in the cortical collecting tubule)
Effects:
1) Acidemia (K+ & H+ retention)
2) NaCl excretion
Clinical uses:
1) Hyperaldosteronism
2) Hypokalemia
3) Heart failure
4) Nephrogenic Diabetes Insipidus
5) Anti-Androgenics
Adverse effects:
1) Hyperkalemia & arrythmia
2) Endocrine symptoms (Gynecomastia)
3) Metabolic acidosis
Describes which group of diuretics?
K+ sparring diuretics that act in the Cortical collecting tubule
Spironolactone
Eplerenone
Amiloride
Triamterene
Are examples of which type of diuretics?
K+ sparring that act in the cortical collecting tubules
K+ sparring that act in the cortical collecting tubules, include which drugs?
Spironolactone
Eplerenone
Amiloride
Triamterene
Describe the following for carbonic anhydrase inhibitors:
What are the drugs?
What is the MOA?
What are the effects?
What are the clinical uses?
What are the Adverse effects?
Drugs:
Acetazolamide
MOA:
It causes self limiting NAHCO3 diuresis & reduced total body HCO3 stores
Effects:
1) Alkalinize the urine
Clinical use:
1) Glaucoma
2) Metabolic alkalosis
3) Altitude sickness
4) Idiopathic intracranial hypertension
Adverse effects:
1) Proximal renal tubular acidosis
2) Paresthesia
3) NH3 toxicity
4) Sulfa allergy
5) Hypokalemia
6) Calcium phosphate stone formation (kidney stones)
Drugs:
Acetazolamide
MOA:
It causes self limiting NAHCO3 diuresis & reduced total body HCO3 stores
Effects:
1) Alkalinize the urine
Clinical use:
1) Glaucoma
2) Metabolic alkalosis
3) Altitude sickness
4) Idiopathic intracranial hypertension
Adverse effects:
1) Proximal renal tubular acidosis
2) Paresthesia
3) NH3 toxicity
4) Sulfa allergy
5) Hypokalemia
6) Calcium phosphate stone formation (kidney stones)
Describes which diuretic type?
Carbonic anhydrase inhibitor
What are the antihypertensives deemed safe for use during pregnancy?
Hydralazine
Labetalol
Methyldopa
Nifedipine
“He Likes My Neonate”
Hydralazine
Labetalol
Methyldopa
Nifedipine
Describes drugs that can be used for what condition?
Hypertension during pregnancy
Describe the following for oprelvekin (IL-11):
What is the drug type?
What is the MOA?
What are the clinical uses?
What are the adverse effects?
Drug type:
A megakaryocyte growth factor
MOA:
It activates IL-11 receptors to stimulate the growth of primitive megakaryocytic progenitors & increase the number of peripheral platelets
Clinical uses:
1) A secondary prevention of thrombocytopenia in patients undergoing cytotoxic chemotherapy for non-myeloid cancer
Adverse effects:
1) Fatigue
2) Headache
3) Dizziness
4) Anemia
5) Plural edema
6) Transient atrial arrythmias
Drug type:
A megakaryocyte growth factor
MOA:
It activates IL-11 receptors to stimulate the growth of primitive megakaryocytic progenitors & increase the number of peripheral platelets
Clinical uses:
1) A secondary prevention of thrombocytopenia in patients undergoing cytotoxic chemotherapy for non-myeloid cancer
Adverse effects:
1) Fatigue
2) Headache
3) Dizziness
4) Anemia
5) Plural edema
6) Transient atrial arrythmias
Describes which drug?
Oprelvekin (IL-11)
Describe the following for folic acid:
What is the MOA?
What is the clinical use?
What is an adverse effect?
MOA:
A precursor of an essential donor of methyl groups used to make amino acids, purines, & deoxynucleotides
Clinical uses:
1) Folic acid deficiency (megaloblastic anemia) to prevent NTD
Adverse effects:
1) Masks B12 deficiency when given in large doses
MOA:
A precursor of an essential donor of methyl groups used to make amino acids, purines, & deoxynucleotides
Clinical uses:
1) Folic acid deficiency (megaloblastic anemia) to prevent NTD
Adverse effects:
1) Masks B12 deficiency when given in large doses
Describes which drug?
Folic acid
Describe the following for Cyanocobalamin (vit B12):
What is the MOA?
What are the clinical uses?
MOA:
A cofactor that is needed for essential enzymatic reactions that form tetrahydrofolate which converts monocysteine into methione & metabolizes methyl-malonyl-CoA
Clinical uses:
1) Vit B12 deficiency (megaloblastic anemia)
2) Pernicious anemia
MOA:
A cofactor that is needed for essential enzymatic reactions that form tetrahydrofolate which converts monocysteine into methione & metabolizes methyl-malonyl-CoA
Clinical uses:
1) Vit B12 deficiency (megaloblastic anemia)
2) Pernicious anemia
Describes which drug?
Cyanocobalamin (vit B12)
Which drugs are considered Ca2+ channel blockers?
Amlodipine
Clevidipine
Nicardipine
Nifedipine
Diltiazem
Verapamil
Amlodipine
Clevidipine
Nicardipine
Nifedipine
Diltiazem
Verapamil
Are all considered which type of drug?
Ca2+ channel blockers
Describe the following for Amlodipine:
What is the drug type?
What is the MOA?
What are the clinical uses?
What are the adverse effects?
Drug type:
Ca2+ channel blocker
MOA:
It blocks voltage dependent L-type Ca2 channels of vascular smooth muscle resulting in relaxation
Clinical use:
1) Hypertension
2) Angina
3) Raynaud syndrome
Adverse effects:
1) Ankle edema (peripheral)
2) Gingival hyperplasia
3) Flushing
4) Dizziness
Drug type:
Ca2+ channel blocker
MOA:
It blocks voltage dependent L-type Ca2 channels of vascular smooth muscle resulting in relaxation
Clinical use:
1) Hypertension
2) Angina
3) Raynaud syndrome
Adverse effects:
1) Ankle edema (peripheral)
2) Gingival hyperplasia
3) Flushing
4) Dizziness
Describes which drug?
Amlodipine
Which Ca2+ channel blockers are considered dihydropyridines?
Amlodipine
Clevidipine
Nifedipine
Nimodipine
They act on relaxing the vascular smooth muscle
Amlodipine
Clevidipine
Nifedipine
Nimodipine
They act on relaxing the vascular smooth muscle are considered to be which type of Ca2+ channel blockers?
Dihydropyridines
Nimodipine is used to treat which condition?
Subarachnoid hemorrhage
Nicardipine & Clevidipine are used to treat which condition?
Hypertension urgency or emergency
What are the non-dihydropyridines & what do they treat?
Diltiazem & Verapamil
They act on the heart
Rx:
1) Hypertension’
2) Angina
3) A fibrillation
4) A flutter
Adverse effects:
1) Cardiac depression
2) AV block
3) Hyperprolactinemia (verapamil)
4) Constipation
Non-dihydropyridines that act on the heart
Rx:
1) Hypertension’
2) Angina
3) A fibrillation
4) A flutter
Adverse effects:
1) Cardiac depression
2) AV block
3) Hyperprolactinemia (verapamil)
4) Constipation
Describes which 2 drugs?
Diltiazem & Verapamil
Describe the following for Sildenafil:
What is the drug type?
What is the MOA?
What are the clinical uses?
What are the adverse effects?
- Avoid giving which drugs?
Drug type:
A PDE-5 inhibitor (phosphodiesterase)
MOA:
It inhibits PDE-5 to increase available cGMP to prolong the vasodilatory effects of nitric oxide
Clinical use:
1) Erectile dysfunction’
2) Pulmonary hypertension
Adverse effects:
1) Headache
2) Flushing
3) Transient blue-green tinted vision
Avoid giving with nitroglycerines or nitrates otherwise you risk severe hypotension
Drug type:
A PDE-5 inhibitor (phosphodiesterase)
MOA:
It inhibits PDE-5 to increase available cGMP to prolong the vasodilatory effects of nitric oxide
Clinical use:
1) Erectile dysfunction’
2) Pulmonary hypertension
Adverse effects:
1) Headache
2) Flushing
3) Transient blue-green tinted vision
Avoid giving with nitroglycerines or nitrates otherwise you risk severe hypotension
Describes which drug?
Sildenafil
Describe the following for Dobutamine:
What is the drug type?
What are the effects of the drug?
What are the clinical uses?
What are the adverse effects?
Drug type:
A B1 selective agonist (B1>B2>a) sympathomimetic
MOA:
It stimulates B1 receptors to activate Gs path to increase adenylate cyclase & cAMP resulting in increased CO without significantly raising the HR
Effects:
1) Increased CO
Clinical uses:
1) Cardiogenic shock
2) Heart failure
3) Cardiac stress test
Adverse effects:
1) Hypertension
2) Tachycardia
3) PVC’s
4) Arrythmias
Drug type:
A B1 selective agonist (B1>B2>a) sympathomimetic
MOA:
It stimulates B1 receptors to activate Gs path to increase adenylate cyclase & cAMP resulting in increased CO without significantly raising the HR
Effects:
1) Increased CO
Clinical uses:
1) Cardiogenic shock
2) Heart failure
3) Cardiac stress test
Adverse effects:
1) Hypertension
2) Tachycardia
3) PVC’s
4) Arrythmias
Describes which drug?
Dobutamine
Describe the following for nitrates:
What are the drugs?
What is the MOA?
What are the clinical uses?
What are the adverse effects?
Drugs:
Nitroglycerin
Isosorbide dinitrate
Isosorbide mononitrate
MOA:
They increase NO & cGMP in smooth muscle & veins resulting in vasodilation & reduced preload in the heart
Clinical uses:
1) Angina
2) Acute coronary syndrome
3) Pulmonary edema
Adverse effect:
1) Reflex tachycardia
2) Methemoglobinemia
3) Hypotension
4) flushing
5) Headache
6) Monday syndrome (exposure during the work week causes sensitization but re-exposure after the weekend makes headache, tachycardia, & dizziness worse)
Drugs:
Nitroglycerin
Isosorbide dinitrate
Isosorbide mononitrate
MOA:
They increase NO & cGMP in smooth muscle & veins resulting in vasodilation & reduced preload in the heart
Clinical uses:
1) Angina
2) Acute coronary syndrome
3) Pulmonary edema
Adverse effect:
1) Reflex tachycardia
2) Methemoglobinemia
3) Hypotension
4) flushing
5) Headache
6) Monday syndrome (exposure during the work week causes sensitization but re-exposure after the weekend makes headache, tachycardia, & dizziness worse)
Describes which drug type?
Nitrates
People with which conditions do you NOT want to give nitrates?
Right ventricular infarction
Hypertrophic cardiomyopathy
People taking PDE-5 inhibitors (Sildenafil)
Describe the RAAS pathway & where each of these drugs inhibit the steps:
1) Mineralcorticoid antagonists (Spironolactone & Eplerenone)
2) ACE inhibitors (-Prils)
3) Direct renin inhibitor (Aliskiren)
4) Angiotension II receptor blockers (-sartans)
5) Aldosterone antagonists
Angiotensin
(Renin) *3) Direct renin inhibitor
angiotensin I
(ACE) *2) ACE inhibitors
Angiotensin II
*4) Angiotensin II receptor blockers
Aldosterone
*5) Aldosterone antagonists
Adrenals
*1) Mineralcorticoid antagonists
Target tissues
Describe the following for procainamide:
What is the drug type?
What is the MOA?
What are the effects?
What are the clinical uses?
What are the adverse effects?
Drug type:
Na channel blocker (antiarrhythmic)
MOA:
A moderate Na channel blocker to increase AP duration to increase the effective refractory period ventricular action potential & it’s metabolized by N-acetyltransferase.
Effects:
1) Increased AP duration
2) Increased QT interval
3) Block some K+
Clinical uses:
1) Atrial & ventricular arrythmias
2) Re-entrant/ectopic SVT & VT
Adverse effects:
1) SLE-like symptoms (SHIPPD acetylation metabolism)
2) thrombocytopenia
3) Torsade’s de points (QT interval)
Drug type:
Na channel blocker (antiarrhythmic)
MOA:
A moderate Na channel blocker to increase AP duration to increase the effective refractory period ventricular action potential & it’s metabolized by N-acetyltransferase.
Effects:
1) Increased AP duration
2) Increased QT interval
3) Block some K+
Clinical uses:
1) Atrial & ventricular arrythmias
2) Re-entrant/ectopic SVT & VT
Adverse effects:
1) SLE-like symptoms (SHIPPD acetylation metabolism)
2) thrombocytopenia
3) Torsade’s de points (QT interval)
Describes which drug?
Procainamide
Describe the following for statins:
What are the drugs?
What is the MOA?
What are the effects of the drug?
What adverse effects?
What are the drugs:
Atorvastatin
Simvastatin
MOA:
They inhibit conversion HMG-CoA to mevalonate (a cholesterol precursor)
Effects:
1) Very low LDL (more LDL receptor recycling & increased expression on hepatocytes to up catabolism)
2) High HDL
3) Low triglycerides (less intrahepatic fat)
Adverse effects:
1) Hepatotoxicity
2) Statin-induced myopathy (especially when given fibrates or niacin)
What are the drugs:
Atorvastatin
Simvastatin
MOA:
They inhibit conversion HMG-CoA to mevalonate (a cholesterol precursor)
Effects:
1) Very low LDL (more LDL receptor recycling & increased expression on hepatocytes to up catabolism)
2) High HDL
3) Low triglycerides (less intrahepatic fat)
Adverse effects:
1) Hepatotoxicity
2) Statin-induced myopathy (especially when given fibrates or niacin)
Describes which type of drug?
Statins
Describe the following for niacin:
What is the drug type?
What is the MOA?
What are the effects?
What are the adverse effects?
Drug type:
A hormone-sensitive lipase inhibitor
MOA:
It inhibits lipolysis in fat to reduce VLDL synthesis in the liver
Effects:
1) Very low LDL
2) Very high HDL
3) Low Triglycerides
Adverse effects:
1) Flushed face
2) Hyperglycemia
3) Hyperuricemia
Drug type:
A hormone-sensitive lipase inhibitor
MOA:
It inhibits lipolysis in fat to reduce VLDL synthesis in the liver
Effects:
1) Very low LDL
2) Very high HDL
3) Low Triglycerides
Adverse effects:
1) Flushed face
2) Hyperglycemia
3) Hyperuricemia
Describes which drug?
Niacin
Describe the following for fibrates:
What are the drugs included?
What is the drug type?
What is the MOA?
What are the effects?
What are the adverse effects?
Drugs:
Gemfibrozil
Bezafibrate
Fenofibrate
Drug type:
PPAR-a activator
MOA:
They activate PPAR-a (peroxisome proliferative factor) to upregulate LPL & increased triglyceride clearance resulting in induced HDL synthesis
Effects:
1) Low LDL
2) High HDL
3) Very low Triglycerides
Adverse effects:
1) Myopathy (especially given with statins)
2) Cholesterol gallstones
Drugs:
Gemfibrozil
Bezafibrate
Fenofibrate
Drug type:
PPAR-a activator
MOA:
They activate PPAR-a (peroxisome proliferative factor) to upregulate LPL & increased triglyceride clearance resulting in induced HDL synthesis
Effects:
1) Low LDL
2) High HDL
3) Very low Triglycerides
Adverse effects:
1) Myopathy (especially given with statins)
2) Cholesterol gallstones
Describes which type of drug?
Fibrates
Gemfibrozil
Bezafibrate
Fenofibrate
Are all examples of which type of drug that works in what way?
Fibrates aka PPAR-a activators that work to reduce LDL & triglycerides & raise HDL
Fibrates aka PPAR-a activators that work to reduce LDL & triglycerides & raise HDL
Gemfibrozil
Bezafibrate
Fenofibrate
Describe the following for digoxin:
What is the drug type?
What is the MOA?
What are the effects?
What are the clinical uses?
What are the adverse effects?
Drug type:
An indirect Na/K+ ATPase inhibitor
MOA:
It inhibits Na+/K+ ATPase meaning there is no Na+ for the Na/Ca2+ exchanger resulting in less available Ca2+ for cardiomyocytes & a stimulated vagus nerve causing reduced HR
Effects:
1) Lower HR, Conduction & Contractility
Clinical uses:
1) Heart failure
2) A fibrillation (reduces conduction at the AV/SA nodes)
Adverse effects:
1) Cholinergic effects (N/V/D)
2) Yellow tinged vision
3) Arrythmias
4) AV block
5) Hypokalemia (poor prognosis)
Drug type:
An indirect Na/K+ ATPase inhibitor
MOA:
It inhibits Na+/K+ ATPase meaning there is no Na+ for the Na/Ca2+ exchanger resulting in less available Ca2+ for cardiomyocytes & a stimulated vagus nerve causing reduced HR
Effects:
1) Lower HR, Conduction & Contractility
Clinical uses:
1) Heart failure
2) A fibrillation (reduces conduction at the AV/SA nodes)
Adverse effects:
1) Cholinergic effects (N/V/D)
2) Yellow tinged vision
3) Arrythmias
4) AV block
5) Hypokalemia (poor prognosis)
Describes which drug?
Digoxin (cardiac glycoside)
Describe the following for Digoxin toxicity::
What are the predisposing factors/risks?
What is the antidote?
Risks:
1) Renal failure
2) Hypokalemia
3) Drugs that displace digoxin from tissues (Verapamil, Amiodarone, Quinidine)
Rx:
Anti-digoxin Fab fragments
Slowly normalize K+
Cardiac pacer (in severe cases)
Mg2+ Supplements
Risks:
1) Renal failure
2) Hypokalemia
3) Drugs that displace digoxin from tissues (Verapamil, Amiodarone, Quinidine)
Rx:
Anti-digoxin Fab fragments
Slowly normalize K+
Cardiac pacer (in severe cases)
Mg2+ Supplements
Describes which type of toxicity?
Digoxin toxicity
Describe the following for ACE inhibitors:
What are the drugs included?
What is the MOA?
What are the effects?
What are the clinical uses?
What are the adverse effects?
Drugs:
Lisinopril*
Ramipril*
Captopril
Enalapril
MOA:
Inhibit ACE to reduce angiotensin II levels resulting in dilation of blood vessels like the efferent arteriole to reduce GFR & BP
Effects:
1) Increase Bradykinin
2) Increase renin
3) Increase K+
4) Increase angiotensin I
5) Reduce Aldosterone
6) Reduce Angiotensin II
Clinical uses:
1) Hypertension
2) Heart failure
3) Proteinuria
4) Diabetic neuropathy
5) Prevent cardiomyopathies via chronic HTN
Adverse effects:
1) Cough
2) Angioedema
3) Teratogenic (Hypoplastic digits, Oligohydramnios, Renal dysplasia)
4) Hyperkalemia
5) Hypotension
“CATCHH”
Drugs:
Lisinopril*
Ramipril*
Captopril
Enalapril
MOA:
Inhibit ACE to reduce angiotensin II levels resulting in dilation of blood vessels like the efferent arteriole to reduce GFR & BP
Effects:
1) Increase Bradykinin
2) Increase renin
3) Increase K+
4) Increase angiotensin I
5) Reduce Aldosterone
6) Reduce Angiotensin II
Clinical uses:
1) Hypertension
2) Heart failure
3) Proteinuria
4) Diabetic neuropathy
5) Prevent cardiomyopathies via chronic HTN
Adverse effects:
1) Cough
2) Angioedema
3) Teratogenic (Hypoplastic digits, Oligohydramnios, Renal dysplasia)
4) Hyperkalemia
5) Hypotension
“CATCHH”
Describes which type of drug?
ACE inhibitors
Describe the following for Sartans:
What are the drugs included?
What is the type of drug?
What are the effects?
What are the clinical uses?
What are the adverse effects?
Drugs:
Losartan**
Candesartan
Valsartan
Drug type:
Selective angiotensin receptor blockers (ARBs)
Effects:
1) NO change in bradykinin
2) Reduced Aldosterone
3) Increased K+
4) Increased Renin
5) Increased Angiotensin I & II
Clinical uses:
1) HTN
2) HF
3) Proteinuria
4) Chronic kidney disease (diabetic neuropathy with intolerance to ACE inhibitors)
Adverse effects:
1) Hyperkalemia
2) Reduced GFR
3) Hypotension
4) Teratogenic effects
Drugs:
Losartan**
Candesartan
Valsartan
Drug type:
Selective angiotensin receptor blockers (ARBs)
Effects:
1) NO change in bradykinin
2) Reduced Aldosterone
3) Increased K+
4) Increased Renin
5) Increased Angiotensin I & II
Clinical uses:
1) HTN
2) HF
3) Proteinuria
4) Chronic kidney disease (diabetic neuropathy with intolerance to ACE inhibitors)
Adverse effects:
1) Hyperkalemia
2) Reduced GFR
3) Hypotension
4) Teratogenic effects
Describes which type of drugs?
Sartans
Which two drugs inhibit norepinephrine reuptake?
Cocaine & Imipramine
Which drug is used to treat BPH & HTN?
Tamsuloin
An irreversible alpha blocker used to treat pheochromocytoma followed by a B-blocker to avoid a hypertensive crisis & arrythmia
Phenoxybenzamine
Nicotinic receptors target which tissues?
CNS & skeletal muscles (ligand-gated ion channels)
M1 & M3 receptors target which secondary messenger pathway?
Gq to increase phospholipase C & IP3, DAG, & Ca2+
M2 & M4 receptors target which secondary messenger pathway?
Gi to decrease adenylate cyclase & cAMP levels
M1 targets which tissues?
CNS
Ganglia
Gastric parietal cells
CNS
Ganglia
Gastric parietal cells
Are all acted upon by which receptor?
M1
M2 targets which tissues?
Heart
Heart
is acted upon by which receptor?
M2
M3 targets which tissues?
Smooth muscle
Eye
GIT
Bronchus
Bladder
Smooth muscle
Eye
GIT
Bronchus
Bladder
Are all acted upon by which receptor?
M3
Describe the following for Albuterol & Salbutamol:
What are the drug types?
What are they clinically used for?
Drug type:
B2 agonist (bronchodilation via M3 receptors)
Clinical use:
1) Acute bronchial asthma
2) Hyperkalemia (B2 causes K+ uptake into SM)
Drug type:
B2 agonist (bronchodilation via M3 receptors)
Clinical use:
1) Acute bronchial asthma
2) Hyperkalemia (B2 causes K+ uptake into SM)
Describes which 2 drugs?
Albuterol & Salbutamol:
Pilocarpine is a direct Muscarinic agonist that can treat which conditions?
Closed-angle glaucoma
Xerostomia (sjogrens)
Miosis (side effect)
Which 2 drugs are the go to when treating open-angle glaucoma’s?
1) Latanoprost (PGF2a receptor to increase uveoscleral outflow)
2) Timolol (non-selective B-blocer that reduced aqueous humor production by blocking B2 receptors)
Which drugs are considered cardio selective B-blockers?
- What are their effects?
- What conditions should you avoid giving them in?
Atenolol & Metoprolol the lol’s
Effects:
1) Bradycardia
2) Fatigue
3) Masked hypoglycemia
Avoid in:
1) Diabetes
2) Asthma/COPD
3) CHF
4) Heart block
What is the first line choice rx for Alzheimer’s & what is the alternative?
1 Rivastigmine (because it has fewer drug interactions)
Alternative:
Donepezil an indirect muscarinic agonist
Describe the following for Atropine:
What is the drug type?
What are the effects?
What is the clinical use?
Drug type:
A direct muscarinic antagonist
Effects: anticholinergic
1) CNS stimulation
2) Raised temperature
3) Mydriasis
4) Dry mouth/flushed dry skin
Rx:
Organophosphate poisoning (insecticides)
Drug type:
A direct muscarinic antagonist
Effects: anticholinergic
1) CNS stimulation
2) Raised temperature
3) Mydriasis
4) Dry mouth/flushed dry skin
Rx:
Organophosphate poisoning (insecticides)
Describes which drug?
Atropine
Describe the following for Physostigmine:
What is the drug type?
What is the clinical use?
Drug type:
An indirect muscarinic agonist (AChE inhibitor)
Rx:
Atropine poisoning
Drug type:
An indirect muscarinic agonist (AChE inhibitor)
Rx:
Atropine poisoning
Describes which drug?
Physostigmine
Which drugs would you give a farmer showing signs of organophosphate poisoning?
Atropine & Pralidoxime
Describe the following for clonidine:
What is the drug type?
What are the effects?
What are the adverse effects?
Drug type:
a2 agonist at prejunctional synapses
Effects:
1) Decreased sympathetic outflow & relaxation of SM/BVs
Adverse effects:
1) Rebound HTN when medication is discontinued
Drug type:
a2 agonist at prejunctional synapses
Effects:
1) Decreased sympathetic outflow & relaxation of SM/BVs
Adverse effects:
1) Rebound HTN when medication is discontinued
Describes which drug?
Clonidine
Describe the following Bethanechol:
What is the drug type?
What is the clinical use?
Drug type:
A direct muscarinic agonist (M3) that frees the pee!
Rx urine retention (contracts bladder wall detrusor)
Drug type:
A direct muscarinic agonist (M3) that frees the pee!
Rx urine retention (contracts bladder wall detrusor)
Describes which drug?
Bethanechol
Describe the following for Oxybutynin:
What is the drug type?
What are the effects?
What is the clinical use?
Drug type:
Muscarinic antagonist (M3)
Effects (relaxes detrusor/bladder wall)
Rx Overactive bladder/incontinence
Drug type:
Muscarinic antagonist (M3)
Effects (relaxes detrusor/bladder wall)
Rx Overactive bladder/incontinence
Describes which drug?
Oxybutynin
M1, M4, M5
Influences neurologic function (e.g., cognitive impairment)
M2
↑ Heart rate
Increases AV-node conduction (may lead to tachyarrhythmia)
M3
- Gastrointestinal tract
↓ Intestinal peristalsis
↓ Salivary and gastric secretions - Urinary tract:
↓ Bladder contraction (↓ detrusor muscle tone, ↑ internal urethral sphincter tone) - Airway
Bronchodilation
↓ Bronchial secretions - Eye
Mydriasis → narrowing of the iridocorneal angle & Impaired accommodation - Blood vessels minimal effect
- Exocrine ↓ Secretions (sweat)
Ipratropium bromide
Tiotropium bromide
List of antimuscarinic agents that are Quarternary amines
Hydrophilic (poor oral bioavailability and CNS penetration)
Atropine
Scopolamine
Homatropine
Tropicamide
Benzotropine
Biperiden
Trihexyphenidyl
Oxybutynin
Tolterodine
Solifenacin
Dicyclomine
Hyoscyamine
Darifenacin
All represent
antimuscarinic agents
List the Tertiary amines that are
Lipophilic (good oral bioavailability and CNS penetration)
Nebivolol (most)
Bextaxolol
Bisoprolol
Acebutolol
Esmolol
Atenolol
Metoprolol
Celiprolol
Are examples of which type of drug that have what effect?
Cardio-selective beta blockers (B1 selective) -lol
Reduces heart rate, contractility, and myocardial oxygen
consumption
What are the adverse effects of cardio selective B-blockers?
Adverse effects
1) Bradycardia*
2) Masks hypoglycemia*
3) fatigue
4) cold extremities
5) sleep disturbances
6) depression
Adverse effects
1) Bradycardia*
2) Masks hypoglycemia*
3) fatigue
4) cold extremities
5) sleep disturbances
6) depression
Are all adverse effects of which type of drug?
Cardioselective B-blockers
Which conditions should you avoid giving cardioselective B-blockers to?
Contraindications
1) Asthma/COPD
2) diabetes
3) heart block/CHF
List the types of drugs that cause Miosis (constriction)
1) Sympatholytic (a2 agonists)
2) Heroin/opioids
3) Parasympathomimetic (pilocarpine)
List the types of drugs that cause Mydriasis (dilation)
1) Anticholinergics
(atropine, TCAs, tropicamide, antihistamines)
2) Drug abuse (amphetamines, cocaine, LSD)
3) Sympathomimetics (Cyclopentolate, homatropine, scopolamine and tropicamide)
What is the MOA of Donepezil
Ach esterase inhibitor
- Increase acetylcholine levels in synaptic cleft
Wha) are the signs of an atropine OD (CNS stimulant)
o Hot as a hare: increased temperature
o Blind as a bat: mydriasis (dilated pupils)
o Dry as a bone: dry mouth, dry eyes, decreased sweat
o Red as a beet: flushed face
o Mad as a hatter: delirium
What is the drug used to treat an atropine OD & why?
Physostigmine (because it crosses the BBB to increase Ach availability to bind muscarinic receptors
What is the presentation of organophosphate poisoning?
What is the treatment?
Insecticides Poisoning (farmers)
Muscarinic effect like dumbbells –
diarrhea, urination, miosis, bradycardia,
bronchoconstriction, lactation, sweating
Treatment –
atropine (lifesaving; crosses BBB)
or
pralidoxime
What is the MOA of clonidine & what is its effect?
What is an adverse effect?
a2 agonist (presynaptic) that reduces of sympathetic outflow from CNS
Antihypertensive effect: can cause rebound hypertension when discontinued
What drug is used to treat urinary retention & why?
Muscarinic agonist like bethanechol that Activates M3 receptor to contract the detrusor smooth muscle & increase bladder emptying
What drug is used to treat urgency incontinence & why?
Muscarinic antagonists LIKE Oxybutynin by Inhibits M3 receptor to relax the detrusor smooth muscle & decrease
overactivity
Sympathomimetics that inhibit synthesis of norepinephrine block which step (& what process is prevented?)
Step A where the hydroxylation of tyrosine is prevented (RLS)
Sympathomimetics that inhibit Uptake of dopamine into storage vesicles block which step (& what process is prevented?)
Step B, drugs like reserpine inhibits transport of dopamine into the vesicles & prevent it from being converted into norepinephrine & being protected from degradation
Sympathomimetics that inhibit Release of neurotransmitter block which step (& what process is prevented?)
Step C, drugs like guanethidine & bretylium block the influx of Ca2+ & exocytosis of norepinephrine
Sympathomimetics that inhibit Binding to receptor block which step (& what process is prevented?)
Step D, it blocks the Postsynaptic receptor from being activated by binding of
neurotransmitter
Sympathomimetics that inhibit Removal of norepinephrine block which step (& what process is prevented?)
Step E, drugs like cocaine & imipramine inhibit norepinephrine reuptake
Norepinephrine is metabolized by which factors?
Norepinephrine is methylated by COMT and oxidized by MAO
Tamsulosin is used to treat which condition
BPH
Phenoxybenzamine is used to treat which condition & prep for what?
used to treat pheochromocytoma
(Beta blockers need to be used secondary to alpha blockers, A then B; Phenoxybenzamine + atenolol to avoid hypertensive crisis)
Used to treat patient preparation for surgery
Nicotinic vs muscarinic receptors
Nicotinic receptors:
– limited to CNS and skeletal muscle (Ligand-gated ion channels)
Muscarinic receptors:
widely distributed (G protein – coupled receptors)
M1 & M3 receptor
Gq coupled – increase
phospholipase C &increase IP3, DAG, and Ca2+
M1 receptors: CNS, ganglia, and gastric parietal cells
M3 receptors: smooth muscle and secretory cells (eye, GIT, bronchus, bladder)
1) Increases contractions and secretory activity of GIT & parasympathetic response
2) In respiratory system & increase tracheobronchial secretion and
bronchoconstriction
M2 and M4
Gi coupled – decrease
adenylyl cyclase & decrease cAMP
M2 receptors: myocardium
1) Decrease rate of conduction in SA & AV nodes
What is the MOA of Zilueton?
What step does it inhibit?
Step C, 5-lipoxygenase pathway inhibitor (HPX)
that blocks the conversion of arachidonic acid into hydroperoxides
What is the MOA of Montelukast? What step does it inhibit?
Step G, a leukotriene receptor antagonist that blocks leukotriene receptors to reduce bronchoconstriction in asthma (HPX)
Treatment of acute bronchial asthma & hyperkalemia
Albuterol and Salbutamol (B2 agonist)
- Question will be presented with potassium levels greater than 5
What are the Bronchodilators uses in asthma
1) Sympathomimetics
Salbutamol, albuterol, terbutaline, orciprenaline, bambuterol
2)Anti-cholinergic (atropine derivatives)
Ipratropium bromide, oxitropium, tiotropium
Carbonic anhydrase inhibitor -ide effects which part of the nephron
In the PCT
o Acetazolamide
Osmotic diuretic includes which drug?
Mannitol
Loop diuretics effects which part of the nephron
thick ascending LoH (loop loses calcium)
Furosemide is given in cases of hypercalcemia; reduces calcium
Increased sodium, potassium, and calcium excretion
Thiazide diuretics effects which part of the nephron
In the DCT
1) Hydrochlorothiazide which given in case of renal stones
Potassium sparing diuretics effects which part of the nephron
In the collecting duct
Amiloride, spironolactone
Digoxin acts on the which transporter to reduce heart contractility?
sodium/potassium
What is the MOA of Lisinopril & what are the effects on lab values
ACE inhibitor
- Increases bradykinin, renin, and AT1
- Low aldosterone and high potassium
What is the MOA of Losartan & what are the effects on lab values
angiotensin receptor blockers
- No effect on bradykinin
- Increases renin, AT1, AT2
- Low aldosterone and high potassium
What is the MOA of Statin & what are the effects on lab values, & adverse effect?
inhibiting HMG-CoA reductase therefore decreasing cholesterol
- Increasing LDL receptor expression on hepatocytes; high LDL clearance
- Statin-induced myopathy
- Highly hepatotoxic drug
What is a side effect of niacin?
Flushed face
What is the MOA of fibrates?
stimulates PPR-a – stimulates lipoprotein lipase (significantly decreases TG)
What is a side effect of procainamide?
drug-induced lupus (SLE) – SHIPD
What is the MOA of Sildenafil
Classification: PDE-5 inhibitor
Mechanism of Action: inhibits PDE-5 leading to increased cGMP resulting in prolonged vasodilatory effect of NO –– pulmonary artery relaxation
What is Dobutamine used to treat & why?
It treats cardiogenic shock because it’s a beta1 specific agonist to Increases heart contraction
What are nitrates used to treat & why?
angina because they cause venous dilation which decreases preload and high doses can reduce the afterload
What is a side effect of Amlodipine?
Ankle edema
What is the MOA of Labetalol & what can it be used to treat in pregnancy?
Antihypertensive drug safe in pregnancy (methyl dopa and hydralazine) HLMN
- Both alpha and beta blocker activity
What is the MOA of Oprelvekin & what is it to used to prevent?
IL-11 (secondary prevention of thrombocytopenia)
signs of pallor and neurological symptoms (tingling or loss of sensation) indicates which deficiency?
Cyanocobalamin/Vit B12 deficiency
What is the MOA of erythropoietin & what are the adverse effects?
MOA: agonist of erythropoietin receptors expressed by red cell progenitors
AE: hypertension, thrombotic complication
What is the MOA of heparin?
binds to antithrombin III to inhibit factor Xa and IIa (thrombin)
causing excessive bleeding, allergy (anaphylaxis), & thrombocytopenia if toxic (protamide sulphate)
What is the MOA of Enoxaparin? What is it contraindicated in?
activate antithrombin III; inhibiting factor Xa and IIa (thrombin)
Contraindicated in renal failure
What drug type is clopidogrel?
An ADP receptor antagonist
Rx:
- OP poisoning
- Atropine poisoning
- Iron poisoning
- OP poisoning =
atropine or pralidoxime - Atropine poisoning = physostigmine
- Iron poisoning = deferoxamine or deferasirox
Rx:
- Aspirin poisoning
- Acetaminophen poisoning
- Digoxin toxicity
- Aspirin poisoning =
sodium bicarbonate; alkalizing urine - Acetaminophen poisoning = acetylcysteine
- Digoxin toxicity =
Digiband antibodies; present with visual changes
Rx:
- Heparin toxicity
- Warfarin
- Heparin toxicity = protamine sulfate
- Warfarin=
Fresh plasma protein or vitamin K
What drug for acute migraine attacks
Sumatriptan
acute attack of gout
Colchicine
What is the MOA of Colchicine & what is it used to treat?
MOA: binds and stabilizes tubulin to inhibit microtubule polymerization
acute attack of gout
closure of PDA
Indomethacin
What is the MOA of Misoprostol & what is it used to prevent?
PGE1 agonist
- Prevention of NSAID-induced peptic ulcers
What is the MOA of Alprostadil & what is it used to prevent?
PGE1 agonist
- Relaxes smooth muscle in ductus arteriosus (maintenance of PDA)
Which uricosuric agents are used to treat chronic gout?
probenecid & sulphinpyrazone (chronic gout)
probenecid & sulphinpyrazone (chronic gout) are both uricosuric agents that are used to treat which condition?
Chronic gout
What is the drug used to treat Allergic rhinitis
second generation antihistamine drug -adine: Loratadine
ALBUTEROL = SABA.
A short-acting β2agonist
that causes relaxation of bronchial smooth muscle. Used as a bronchodilator.
β2 agonist activates Na+/K+ ATPase channel = help treat hyperkalemia.
SALMETEROL = LABA.
A long-acting β2 adrenergic agonist used to treat COPD and moderate/severe chronic asthma.
Methylxanthines, what is their MOA & effects?
Methylxanthines like theophylline
it causes bronchodilation by inhibiting phosphodiesterase but it has a narrow rx window (neuro/cardio toxicity)
- Hydrochlorothiazide acts on which part & has what effect on Na/K+/Ca2+ excretion?
4 DCT
Decreased Ca2+ excretion
*Furosemide acts on which part & has what effect on Ca2+ excretion?
3 Thick ascending limb of loop of henle
Na/K+/Ca2+ excretion increased
