Drugs - Midterm 2 Flashcards
hydrochlorthiazide
category: thiazide diuretic (anti-hypertensive drug)
mechanism: works on distal convoluted tubule to increase sodium and water excretion, which lowers blood volume.
side effects: hypokalemia (need to eat bananas); glucose intolerant
can be inhibited by NSAIDs under certain conditions.
chlorthalindone
category: thiazide diuretic (anti-hypertensive drug)
mechanism: works on distal convoluted tubule to increase sodium and water excretion, which lowers blood volume.
side effects: hypokalemia (need to eat bananas); glucose intolerant
can be inhibited by NSAIDs under certain conditions.
furosemide
loop diuretic (anti-hypertensive)
mechanism: works on the thick ascending limb to cause a larger increase in urine output (compared to thiazide diuretics). Also more potent and more side effects.
side effects: hypokalemia
can be inhibited by NSAIDs
bumetanide
loop diuretic (anti-hypertensive)
mechanism: works on the thick ascending limb to cause a larger increase in urine output (compared to thiazide diuretics). Also more potent and more side effects.
side effects: hypokalemia
can be inhibited by NSAIDs
spironolactone
- aldosterone antagonist (anti-hypertensive)
- mechanism: works on the collecting duct/tubule to block aldosterone and increase excretion of sodium and water. This drug is potassium sparing…which is why it is often combined with loop diuretics of thiazides. Not used with ACE inhibitors because it can cause worse hypokalemia.
- side effects: head ache, diarrhea, hyperkalemia, electrolyte imbalance, fatigue, GI disturbance
amiloride
- aldosterone antagonist (anti-hypertensive)
- mechanism: works on the collecting duct/tubule to block aldosterone and increase excretion of sodium and water. This drug is potassium sparing…which is why it is often combined with loop diuretics of thiazides. Not used with ACE inhibitors because it can cause worse hypokalemia.
- side effects: head ache, diarrhea, hyperkalemia, electrolyte imbalance, fatigue, GI disturbance
triamterene
- aldosterone antagonist (anti-hypertensive)
- mechanism: works on the collecting duct/tubule to block aldosterone and increase excretion of sodium and water. This drug is potassium sparing…which is why it is often combined with loop diuretics of thiazides. Not used with ACE inhibitors because it can cause worse hyperkalemia.
- side effects: head ache, diarrhea, hyperkalemia, electrolyte imbalance, fatigue, GI disturbance
mannitol
osmotic agent/diuretic (anti-hypertensive)
mechanism: works on the thin descending limb
acetazolamine
diuretic (anti-hypertensive)
mechanism: carbonic anhydrase inhibitor that works in the renal glomerulus
propranolol
- non-selective beta blocker
- reduces peripheral vascular resistance and also reduces cardiac function (decreases HR, BP, and contractility to decrease O2 requirements)
- tx: HTN, angina, arrhythmias
- toxicity: asthma and acute heart failure
can also be used to treat hyperthyroidism: inhibits the conversion of T4 to T3
antenolol
- beta 1 selective inhibitor
- reduces peripheral vascular resistance and also reduces cardiac function (decreases HR, BP, and contractility to decrease O2 requirements)
- tx: HTN, angina
- less risk for bronchospasms
- toxicity: asthma and acute heart failure
metoprolol
- beta 1 selective inhibitor
- reduces peripheral vascular resistance and also reduces cardiac function (decreases HR, BP, and contractility to decrease O2 requirements)
- tx: HTN, angina, heart failure
- less risk for bronchospasms
- toxicity: asthma and acute heart failure
prazosin
- alpha 1 selective inhibitor
- decrease peripheral resistance
- tx: HTN
phentolamine
- alpha 1/2 non-selective inhibitor
- tx: HTN
phenoxybenzamine
- alpha 1/2 non-selective inhibitor
- tx: HTN
clonidine
- alpha 2 agonist
- centrally acting
- tx: HTN
labetalol
- beta 1/2 and alpha 1 antagonist
- tx: HTN
guanethidine
- inhibits release of NE from sympathetic nerve endings (works by depleting NE stores)
- tx: HTN
hydralazine
- arteriole dilator (direct vasodilator)
- hyperpolarizes smooth muscle by opening K+ channels
- tx: HTN, heart failure
minoxidil
- arteriole dilator (direct vasodilator)
- hyperpolarizes smooth muscle by opening K+ channels
- tx: HTN
diazoxide
- arteriole dilator (direct vasodilator)
- tx: HTN
nitroprusside
- arteriole dilator (direct vasodilator)
- tx: HTN
nitroglycerin
- arteriole dilator (direct vasodilator)
- tx: HTN, angina
- administered sublingual
- metabolized to nitric oxide –> increase cGMP –> relax smooth muscle and dilate cardiac vessels
- volatile
- available in long-lasting patches (8hr)
- side effects: orthostatic hypotension, tachycardia, throbbing headache, tolerance
verapamil
- calcium channel blocker
- causes vasodilation (blocks contraction of smooth muscle), and reduces O2 demand, prolongs refractory time
- tx: HTN, angina (prophylaxis), and arrhythmias
- toxicity: cardiac depression and bradycardia, heart failure
dilitiazem
- calcium channel blocker
- causes vasodilation (blocks contraction of smooth muscle), and reduces O2 demand, prolongs refractory time
- tx: HTN, angina, and arrhythmias
- toxicity: cardiac depression and bradycardia, heart failure
captopril
- ACE inhibitor
- blocks angiotensin II
- increases bradykinin (vasodilation)
- side effects: dry cough or hyperkalemia if combined with K+ sparing drugs
- tx: HTN, heart failure
mecamylamine
- ganglion blocker (blocks sympathetic and parasympathetic NS
- rare used due to serious side effects
mechanisms for anti-anginal drugs
vasodilation (increase blood flow and O2)
decrease O2 consumption
amyl nitrate
- anti-anginal (nitrate)
- crushed ampule and fumes are inhaled
- side effects: orthostatic hypotension, tachycardia, throbbing headache, tolerance
nifedipine
- calcium channel blocker
- causes vasodilation (blocks contraction of smooth muscle), and reduces O2 demand
- tx: HTN, angina (prophylaxis)
- toxicity: cardiac depression and bradycardia, heart failure
treatments for lowering lipids or cholesterol
- non-drug (diet and exercise)
2. drugs (diet should still be managed, avoid pregnancy)
Lovastatin
- “Mevacor”
- statins - competitive inhibitor of HMG-CoA reductase to inhibit cholesterol synthesis
- most effect on LDLs and some decrease in triglycerides –> reduces coronary events
- toxicity: liver damage, weakness in skeletal muscles
Atorvastatin
- “Lipitor”
- statins - competitive inhibitor of HMG-CoA reductase to inhibit cholesterol synthesis
- most effect on LDLs and some decrease in triglycerides –> reduces coronary events
- toxicity: liver damage, weakness in skeletal muscles
Simvastatin
- “Zocor”
- statins - competitive inhibitor of HMG-CoA reductase to inhibit cholesterol synthesis
- most effect on LDLs and some decrease in triglycerides –> reduces coronary events
- toxicity: liver damage, weakness in skeletal muscles
Fenobrate
- “Tricor”
- fibrate drug
- increases lipolysis in liver and muscles
- reduces VLDL, modest effect on LDL, and moderate increase in HDL, reduces triglycerides
- toxicity: GI symptoms
Niacin
- nicotinic acid
- decreases triglycerides and LDLs
- side effects: flushing, tolerance develops
cholesteramine
- bile acid binding agent
- reduces absorption of bile acids and metabolites
- side effects: constipation and bloating
exetimibe
- inhibits intestinal sterol absorption
- reduces LDL
digitalis
- positive ionotropic drug
- increase intracellular Ca2+ and cardiac contractility –> increases blood ejection
- side effects: premature depolarization (arrhythmias), ectopic beats, effects in all excitable tissues
milrinone
- positive ionotropic drug
- increase intracellular Ca2+ and cardiac contractility –> increases blood ejection
- side effects: premature depolarization (arrhythmias), ectopic beats, effects in all excitable tissues
dobutamine
- beta 1 agonist
- can cause arrhythmias
How can diuretics be used to treat heart failure?
they reduce salt and water retention which reduces venous pressure and decreases ventricular preload
Procainamide
- Na+ channel blocker (slows action potential conductance)
- tx: atrial and ventricular arrhythmias
- side effects: can precipitate new arrhythmias
- almost never the first choice
Quinidine
- Na+ channel blocker (slows action potential conductance)
- tx: atrial and ventricular arrhythmias
- side effects: can precipitate new arrhythmias
Lidocaine
- Na+ channel blocker (slows action potential conductance)
- tx: atrial and ventricular arrhythmias (usually first choice for ventricular)
- low toxicity
Amiodarone
- prolongs the refractory period
- tx: ventricular arrhythmias and atrial fibrillation
- side effects: pulmonary fibrosis
Rosuvastatin
- “Crestor”
- statins - competitive inhibitor of HMG-CoA reductase to inhibit cholesterol synthesis
- most effect on LDLs and some decrease in triglycerides –> reduces coronary events
- toxicity: liver damage, weakness in skeletal muscles
heparin
- anti-clotting agent, usually used in hospital setting
- affects the INTRINSIC clotting pathway by binding to factor III –> inhibits thrombin
- side effects: hemorrhage, allergic reactions, osteoporosis, bone fractures
- neutralized by protamine binding
enoxaparin
- heparin fraction
- heparin-like drug frequently prescribed to treat deep vein thrombosis
- has fast onset (minutes)
warfarin
- “Coumadin”
- anti-clotting agent
- affects the EXTRINSIC clotting pathway (works through factor VIIa and leads to Xa)
- antagonizes Vitamin K
- side effects: hemorrhage, numbness, pain, headache, dizziness
- oral warfarin is used for outpatient
- need to watch amount of vitamin K in diet (leafy greens)
- slow onset (the drug is used chronically)
Dabigatran
- “Pradaxa”
- alternative drug for warfarin used to treat deep vein thrombosis
- fewer side effects and more popular
- affects PTT sensitive pathway, but has mechanism distinct form warfarin or heparin
- used on outpatient basis
Abciximab
- glycoprotein inhibitor used to prevent clot formation in patients with unstable angina.
Bivalirudin
- “Abjiomax”
- anti-clotting agent
- thrombin inhibitor
- rapid acting and inhibits circulating thrombin
Rivaroxaban
- “Xarelto”
- anti-clotting agent
- oral factor Xa inhibitor
- rapid onset and shorter half-life than warfarin
Streptokinase
- thrombolytic
- anti-clotting agent
- can recanalzie an occluded coronary artery by dissolving the clot.
Aspirin
- cox 1 inhibitor that has anti-platelet effects
drugs to stop bleeding
vitamin K or pure clotting factors
drugs/factors that increase RBC production or decrease anemia
B12 and folic acid
iron
erythropoietin
insulin Lispro
- “Humalog”
- rapid-onset insulin, early peak action, 4 hr duration
- taken immediately before a meal
crystalline zinc insulin
- 30 min. onset, peak in 2-3 hr, lasts 5-8 hr
- “Humulin R” = fast acting
- the zinc helps to delay onset and lengthen duration
NPH (neutral protein hagedorn)
- intermediate acting insulin
- insulin linked to protein called protamine (delayed absorption and onset after injection)
- onset 2-5 hr, duration 4-12 hr
- often mixed with shorter acting insulins
insulin glargine
- long acting sustained insulin, no peak/valleys
- good for background insulin
insulin detemir
long-acting insulin good for background
T/F insulin can be effectively administered PO
False, it is administered subcutaneously
side effects of too much insulin
Hypoglycemia, which leads to: - tachycardia - sweating - tremors - hunger - confusion - seizures - coma Also see local irritation and subdermal atrophy at injection sites.
T/F insulin is usually given to type II diabetics as a first choice to manage glucose levels
False; insulin is given to type II diabetics if glucose levels cannot be managed with oral hypoglycemic drugs first
tolbutamide
- “Orinase”
- 1st generation sulfonylurea
- block K+ channels which in turn increases Ca2+ influx and increases insulin release from beta cells
- bind to plasma proteins in the blood for transport (can be dislodged by other drugs that bind at the same site)
- side effects: hypoglycemia, weight gain
glipizide
- 2nd generation sulfonylurea
- block K+ channels which in turn increases Ca2+ influx and increases insulin release from beta cells
- less protein binding
- side effects: hypoglycemia, weight gain
glitinides
- “Prandin”
- sulfonylurea
- block K+ channels which in turn increases Ca2+ influx and increases insulin release from beta cells
- side effects: hypoglycemia, weight gain
metformin
- biguanides (tx of diabetes); also metformin-glucophage?
- very popular
- decrease glucose production in liver and increase efficiency of insulin binding
- no effect on insulin production in the pancreas
- insulin-sparing (does not provoke hypoglycemia when used alone)
- may prevent some of the CVS effects of type II DM
- side effect: GI irritation, don’t use in alcoholics
Sitagliptin
- “Januvia”
- DPP-4 inhibitor
- slows inactivation of incretin hormones –> stimulates insulin synthesis and release (by prolonging the effects of GIP and glucagon-like peptide 1)
- reduces glucagon activity leading to less hepatic glucose production and release
Acarbose
- tx of diabetes
- alpha-glucosidase inhibitor
- slows digestion/absorption of starch disaccharides from small intenstines (may help to prevent type II DM)
- side effects: GI irritation and bloating, flatulence!
Rosiglitazone
- “Avandia”
- drug class: Thiazolidinediones
- reduces insulin resistance especially in muscles and fat cells by increasing GLUT-4 expression
- tx: type II DM
Glucagon
- used to treat severe hypoglycemia associated with diabetes drugs
- produced in alpha cells of pancreas
- increases gluconeogenesis
Phentermine
- amphetamine used to as an appetite suppressant/weight loss drug
- inhibits norepinephrine and dopamine uptake
- side effects: weight loss, dry mouth, hypertension, palpitation
- interactions with sympathomimetics (including the epi in local anesthetics), MAOIs, SSRIs, and CNS stimulants
Topiramate + phentermine
- “Qsymia”
- anti-convulsant (anti seizure drug)
- weight loss drug
Orlistat
- lipase inhibitor that decreases fat absorption in the intestines
- weight loss drug
Belviq
- “Lorcaserin”
- 5HT2 agonist
- suppresses appetite in the hypothalamus
Propylthiouracil (PTU)
- tx: hyperthyroidism (Grave’s disease)
- drug class: thiomides
- inhibit thyroid peroxidase reaction and blocks the synthesis of thyroid hormone
Lugol solution
- tx: hyperthyroidism
- drug class: Iodides
- inhibits thyroid hormone release
Radioactive iodine
- tx: hyperthyroidism
- destroys thyroid parenchyma
synthroid or levothroid
- thyroid replacement therapy for hypothyroidism
- “Levothyroxine” (T4)
- “Liothyronine” (T3)
denosumab
- “XGEVA”
- tx: osteoporosis
- antibody to osteoclast-stimulating protein “RANK”
- blocks osteoclast number and activity
teraparatide
- “Forteo”
- tx: osteoporosis
- a recombinant form of parathyroid hormone segment which selctively activates osteoblasts and stimulates new bone formation
Estrogens/estrogen modulators for treatment of osteoporosis…
- prevents bone loss in early postmenopausal period
- should be used in combo with progestin to prevent venous thrombi in postmenopausal women
Ibandronate
- “Boniva”
- bisphosphonate
- tx: osteoporosis
- suppress activity of osteoclasts and inhibit bone resorption
- interferes with boney repair after surgery esp. in jaws –> MRONJ
Alendronate
- “Fosamax”
- bisphosphonate
- tx: osteoporosis
- suppress activity of osteoclasts and inhibit bone resorption
- interferes with boney repair after surgery esp. in jaws –> MRONJ
primary uses and side effects of glucocorticoids
- use - rapid and dramatic anti-inflammatory effects (suppress leukocytes and cytokines, topical can inhibit histamine release and skin thinning)
- loss of muscle mass/muscle weakness
- thinning of skin
- impaired wound healing
- osteoporosis
- diabetogenesis (increased blood glucose with increased insulin release as a result)
- peptic ulcers
- catabolic/anti-anabolic effects
Hydrocortisone
- short to medium acting glucocorticoid
- uses: allergic reactions, inflammatory bowel disease, ARDS, dermatitis
- used to treat Addison’s disease (daily dose with an increase during stress, need to combine with a salt-retaining hormone)
cortisone
- short to medium acting glucocorticoid
- uses: allergic reactions, inflammatory bowel disease, ARDS, dermatitis
prednisone
- short to medium acting glucocorticoid
- uses: allergic reactions, inflammatory bowel disease, ARDS, dermatitis
dexamethasone
- long-acting glucocorticoid
- uses: allergic reactions, inflammatory bowel disease, ARDS, dermatitis
ketoconazole
- inhibits adrenal steroid synthesis
- tx: Cushing’s disease
Metyrapone
- selective inhibitor of cortisol/corticosteroid synthesis
- tx: osteoporosis and Paget’s disease (can block osteoblastic bone formation and inhibit vit. D-stimulated intestinal absorption of calcium)
albuterol
beta-2 agonist
“reliever”
rapid onset and 4-6 hr effects
MOA = directly relaxes airway smooth muscle and causes bronchodilation; also decreases microvascular leakage
salmeterol
beta-2 agonist
“reliever”
slower onset than albuterol, 12 hr effectiveness
MOA = directly relaxes airway smooth muscle and causes bronchodilation; also decreases microvascular leakage
fluticasone
inhaled steroid
MOA = anti-inflammatory effects reduce bronchial reactivity
side effects = nose bleeds; sores in nose, mouth, and tongue that don’t heal; increased oral infections (candidiasis)
[oral steroids such as prednisone are last resort]
theophylline
methylxanthine drug (tablet or inhaler) MOA = phosphodiesterase inhibitor that increases cAMP and relaxes airway smooth muscle side effects = headaches, nausea, anxiety, sleep problems uses = add-on controller; monotherapy for mild asthma; combined with corticosteroids to reduce steroid doses and side effects.
ipratropium
anti-muscarinic
MOA = reverses the contraction of smooth muscle and reduces mucous secretions from vagal activity
uses = back-up to beta-2 agonists
slow onset
montelukast
“Singulair”
leukotriene modifier
MOA = block leukotriene-binding receptor
uses = for prophylaxis and for patients that have trouble with inhaled therapies
cromolyn
inhibits releases of inflammatory mediators such as histamine
for prophylactic use only
omalizumab
monoclonal antibodies
inhibit IgE binding to mast cells preventing the release of inflammatory mediators
very expensive
only for severe non-responsive asthma
tiotropium bromide
“Spireva”
Treatment of COPD
long-acting bronchodilator
pharmacological treatment of COPD
- tiotropium bromide - long-acting vasodilator
- salmeterol - longer acting beta-2 agonist
- Theophylline + glucocorticoids
Typically, responses are not as good as with asthma.
oseltamivir
“Tamiflu”
MOA = prevents separation of virus particle from cell receptors –> stops viral spread; early treatment is essential
decreases duration by 1-2 days and reduces severity
effective for both influenza A & B.
diphenhydramine
“Benadryl”
anti-histamine
chlorpeniramine
anti-histamine
epinephrine (for allergy)
potent reversal
vasoconstriction and reduces fluid in the lungs so breathing improves and swelling reduces.
anti-smoking medications
nicotine replacement therapy
bupropion (Zyban; Wellbutrin) - antidepressants
varenicline (Chantix) - stimulates selective nicotine receptors to reduce craving
bupropion
“Zyban”
“Wellbutrin”
anti-depressants
anti-smoking
varenicline
“Chantix”
stimulates selective nicotine receptors to reduce craving
anti-smoking
pharmacological treatment of kidney stones
hydrochlorothiazide - thiazide diuretic; reduces calcium in the urine
sodium bicarbonate - alkalinizes urine
allopurinol - reduces uric acid excretion; also used to gout
Common treatments for UTIs
Trimethoprim-sulfamethoxazole
amoxicillin + clavulanic acid (resistant bacteria can be a problem)
ciprofloxacin (expensive)
