Highlights for the Final Flashcards
What sort of drug will more readily cross plasma membranes?
small, non-ionized, lipid soluble drugs
therapeutic index (TI) is
a ratio of the dose of a drug that produces toxicity relative to the dose of the same drug that produces a clinically desired response. Looked at as an equation, this would be T.I. = LD50 / EC50…thus a measure of the drug’s safety. A large value indicates that there is a wide margin between an effective dose and a toxic dose.
Which drug class has a high potential for abuse?
Class II
Stage 2 HTN
160-179/100-109
Stage 3 HTN
>180/110
What catalyzes angiotensinogen to angiotensin I
renin, a proteolytic enzyme formed in the granules of juxtaglomerular cells
Angiotensin I goes to Angiotensin II by being cleaved by
ACE (angiotensin converting enzyme) which is found mostly in the lungs but also the kidneys and brain and elsewhere
most potent vasoconstrictor produced by the body
angiotensin II
how do thiazide diuretics work
increase sodium and water excretion into urine by inhibiting sodium and chloride reabsorption in the cortical thick ascending limb and early distal tubule
side effect on minerals when taking thiazide diuretics
can cause calcium and uric acid to be reabsorbed by proximal tubule in increased amounts…so serum levels of calcium and uric acid rise
Primary thiazide diuretic
hydrochlorthiazide (HCTZ)/hydrodiuril
what supplement is generally recommended when taking hydrochlorthiazide/hydrodiuril
potassium
patients with a sulfa allergy should not take these drugs because they contain a sulfonamide moiety
hydrochlorthiazide (HCTZ)/hydrodiuril and furosemide/lasix
main loop diuretic
furosemide/lasix
what do loop diuretics do
inhibit chloride reabsorption in the ascending loop of Henle by blocking the Na+/K+/Cl- co-transporter system
***Rank diuretics from strongest to weakest
***loop > thiazide > potassium sparing?
loop diuretics can increase the loss of
sodium, potassium, calcium, and magnesium
bioavailability is
fraction of administered drug that reaches systemic circulation in an unchanged form…(if 100 mg of a drug is taken orally and 70 mg of the drug is absorbed unchanged, then the bioavailability of that drug is 70%)
half life is
the amount of time required for the plasma concentration of a drug to decrease by 50% after discontinuation of a drug
the EC50 or effective concentration 50 is
the concentration or dosage of an agent which induces a specified clinical effect in 50% of the subjects to which the drug has been administered.
LD50 or lethal dose 50 is
the concentration or dosage of an agent or drug which causes death in 50% of the subjects to which that agent or drug has been administered.
efficacy refers to
the degree to which a drug is able to induce maximal therapeutic effects. Efficacy is a term often used to compare drugs of different classes.
drug class with no approved medical use
Class I
drug class with moderate potential for abuse
Class III
drug class with low potential for abuse
Class IV
drug class contraindicated in pregnancy
Class X
preferred diuretic for patients with renal disease and HTN emergencies
loop diuretics
what do potassium sparing diuretics do
increase sodium excretion and inhibit potassium secretion in the distal convoluted tubule
examples of disease states the potassium sparing diuretics should not be used with
severe renal insufficiency, poorly controlled DM, and multiple myeloma
drugs that can cause hyperkalemia
ACE inhibitors and Angiotensin II receptor blockers
primary potassium sparing diuretic
spironolactone/aldactone
diuretic that has anti-androgenic properties and is thus used to treat hirsutism and PCOS
spironolactone/aldactone
prototype B-blocker
propranolol/inderal
beta blocker that acts at both Beta 1 (heart) and Beta 2 (lungs)
propranolol/inderal
beta blocker that is selective (acts at Beta 1)
atenolol/tenormin
disadvantage of B-blockers include
high incidence of adverse CNS affects, sexual dysfunction in men/women, and bradycardia
contraindications of beta blockers include
certain cardiac conduction abnormalities, severe asthma, and severe COPD
drug where abrupt withdrawal can lead to rebound HTN and/or rebound tachycardia, probably due to up-regulation of beta receptors during treatment…can result in MI or stroke
beta blockers
overuse of a beta blocker can result in
bradycardia and heart block
treatment of choice to reverse bradycardic effects of a beta blocker is
glucagon
first line treatment of HTN in conventional clinical practice
ACE inhibitors and calcium channel blockers
treatment for acute asthmatic attacks that are unresponsive to other medications
epinephrine (adrenalin)
indication of epinephrine
emergent treatment of asthma, status asthmaticus, anaphylaxis
OTC preparation containing a very low dose of epinephrine
what is primatene mist
class of albuterol/ventolin, proventil
beta 2 agonist
long acting beta 2 agonist
class of salmeterol/severent
when are anticholinergic drugs typically indicated
generally not indicated for acute asthma attacks but rather for maintenance therapy in asthma patients who cannot tolerate treatment with a beta agonist
primary anticholinergic drug
ipratropium/atrovent
class of zafirlukast/accolate
leukotriene receptor antagonist
drug for prophylaxis and treatment of chronic asthma
zafirlukast/accolate
how do corticosteroids work
inhibition of phospholipase A2 blocks release of arachadonic acid, the precursor of the prostaglandins and leukotrienes from membrane bound phospholipids. Histamine release and kinin activity is also suppressed by glucocorticoids.
primary inhaled steroid
beclomethasone/beclovent, vanceril
indication of beclomethasone/beclovent
asthma not controlled by sympathomimetics (bronchodilators) alone
indication for prednisone/deltasone
COPD, worsening asthma
Abrupt withdrawal of prednisone or other drugs with corticosteroid properties may result in severe and potentially life threatening
hypofunction of the adrenal glands, also known as Addisonian crisis.
What’s significant about theophylline/theo-dur
bad TI, lethal dose is not far from effective dose
class of theophylline/theo-dur
xanthine or methylxanthine bronchodilators
class of codeine
narcotic analgesic and cough suppressant
MOA of codeine and dextromethorphan
suppresses the sensitivity of CNS cough centers in the medulla
Class of dextromethorphan
synthetic derivative of morphine
indication of dextromethorphan
cough suppression
MOA of diphenhydramine/benadryl
H1 receptor site blockage. The production and release of histamine is not blocked.
Does diphenhydramine/benadryl cross the BBB
yes
primary non-sedating antihistamine
loratadine/claritin
MOA of loratadine/claritin
H! receptor antagonist
Does loratadine/claritin
No
Mechanisms of varenicline/chantix
partial agonist of alpha 4/beta 2 nicotinic acetylcholine receptor sites`
side effects of varenicline/chantix
increasing reports of neuro-psychiatric symptoms that range from nightmares or insomnia to depression and suicidal ideations to increased agitation and rage
primary alpha blocker
prazosin/minipress (alpha 1)
indication of prazosin/minipress (alpha 1)
HTN, BPH
Drug class used as prophylaxis of migraine headache and for Raynaud’s syndrome
calcium channel blockers
calcium channel blockers should be used with more caution in patients with
Bradycardia or severe CHF
class of verapamil/isopten
calcium channel blocker
indication of verapamil/isopten
HTN, angina–especially vasospastic angina, CHF
long term use of calcium channel blockers is associated with increased risk for
breast cancer
ACE inhibitors reduce BP by
interfering with the generation of Angiotensin II from Angiotensin I…also inhibit the degradation of bradykinins, allowing for another mechanism by which peripheral vascular resistance can be reduced
what drug is considered least likely of the antihypertensive drugs to cause sexual dysfunction in males
ACE inhibitors
How do ACE inhibitors affect serum lipids, glucose or uric acid levels
They don’t affect them
ACE inhibitors can potentially increase serum
potassium
drug of choice for HTN patients with diabetes
ACE inhibitors
With ACE inhibitors, avoid concurrent use of
potassium sparing diuretic…but potassium wasting diuretics are quite commonly used in conjunction
drug class with the side effect of dry irritating cough
ACE inhibitors
Can you use ACE inhibitors during pregnancy
No
drug class with side effect of angioedema, life threatening when it involves the tongue and oropharyngeal area
ACE inhibitors
Primary ACE inhibitor
Lisinopril/Prinivil or Zestril
Do Angiotensin II receptor blockers cause cough and angioedema
Yes, although their potential to do so is less than ACE Inhibitors
Do Angiotensin II receptor blockers cause hyperkalemia?
Yes
primary Angiotensin II receptor blocker
Losartan/Cozaar
Can you take Losartan/Cozaar during pregnancy
Yes
example of a direct vasodilator
Minoxidil/Loniten
Minoxidil and Hydralazine is generally reserved for
severe hypertension, resistant to previous antihypertensive treatment attempts
What is the more potent direct vasodilator: Minoxidil or Hydralazine?
Minoxidil is more potent than Hydralazine but it is associated with more adverse effects, including potential for marked sodium and water retention and hirsutism
Drug that causes Hirsuitism
Minoxidil/Loniten
drug that causes drug induced lupus syndrome
Hydralazine
first drug FDA approved in new antihypertensive drug class known as direct renin inhibitors
Aliskiren (Tekturna)
drug that can cause angioedema
Aliskiren (Tekturna)
three main classes of drugs that have proven very effective in treating patients with stable angina pectoris
nitrates, beta blockers, calcium channel blockers
the treatment of choice to reverse the bradycardic effects of a beta blocker is
glucagon
Class of propranolol/inderal
non-selective beta blocker
drug used for panic attacks
propranolol/inderal
class of atenolol/tenormin
selective beta blocker
treatment of choice to reverse the symptomatic effects of bradycardia of a calcium channel blocker is
calcium gluconate…but glucagon can be given if calcium gluconate increases pulse rate
class of amlodopine/norvasc
calcium channel blocker
what do you do with someone with unstable angina
administer MONA = morphine, oxygen, nitrate, aspirin
how do you reverse morphine
naloxone
MOA for aspirin/ASA
Irreversibly inhibits cyclooxgenase enzyme. Inhibition of cyclooxgenase prevents the formation of thromboxane A2 and prostaglandins with resultant diminished platelet aggregation.
Drug w markedly increased risk for the development of Reye’s syndrome in children with fevers due to viral conditions such as mumps or chickenpox
aspirin/ASA
what can be used in patients who are intolerant or allergic to aspirin
ADP receptor antagonists
class of Clopidogrel/ Plavix
platelet aggregation inhibitor
what do Glycoprotein IIB/IIIA inhibitors do
prevent the binding of fibrinogen, thereby blocking platelet aggregation.
class of Abciximab/ ReoPro
glycoprotein IIB/IIIA inhibitor
how does regular weight heparin act as an anti-coagulant
Regular weight heparin acts as an anti-coagulant by binding to antithrombin III. The heparin-antithrombin III complex then binds to and inactivates activated factor X (Xa) and factor II (thrombin). Heparin ultimately acts to prevent conversion of fibrinogen to fibrin. Heparin does not actively lyse clots but is able to inhibit further thrombogenesis.
What reverses the effects of heparin
Protamine sulfate
how does low molecular weight heparin act
directly inactivates factor X (Xa) in the clotting cascade…proven to be as effect as regular weight Heparin but with fewer reported side effects
class of Enoxaparin/ Lovenox
low molecular weight heparin
MOA of Warfarin/Coumadin
Antagonizes vitamin K. This interferes with the synthesis of vitamin K dependent clotting factors (factors II, VII, IX, and X).
Anti-coagulant effects of Coumadin may be reversed with
Vit. K
Coumadin should not be used by
Pregnant women
class of Rivaroxaban/ Xarelto
anticoagulant
MOA of Rivaroxaban/Xarelto
direct inhibiton of factor Xa
class of streptokinase
Thrombolytic (clot buster)
Antidote to bleeding in the class of drugs known as “clot busters” (streptokinase)
Aminocaproic acid (Amicar) is a plasmin in-activator and antifibrinolytic. It is utilized for bleeding that occurs as a result of streptokinase and other agents in this class of drugs referred to as the “clot busters”.
anti-arrhythmic drug class Ia, Ib, Ic
sodium channel blockers
anti-arrhythmic drug class II
beta adrenergic receptor blockade
anti-arrhythmic drug class III
potassium channel blockade
anti-arrhythmic drug class IV
calcium channel blockade
class of Quinidine/Quinidex
anti-arrhythmic–Class Ia
MOA of Quinidine/Quinidex
sodium channel blocker
drug that causes Cinchonism
Quinidine/Quinidex
symptoms of cinchonism include
blurred vision, tinnitus, nausea, vomiting, headache, disoreintation and possible psychotic states
drug that may induce Torsade de Pointes
Quinidine/Quinidex
Class of Mexiletine/Mexitil
anti-arrhythmic Class Ib
MOA of Mexiletine/Mexitil
blocks open sodium channels
Class of Flecainide/ Tambocor
anti-arrhythmic Class Ic
drug to treat Wolff-Parkinson-White syndrome
Flecainide/ Tambocor
MOA of Flecainide/ Tambocor
sodium channel blocker
therapeutic index of Flecainide/ Tambocor
narrow
primary Class II/Beta Blocker
Atenolol/Tenormin
Primary Class III/K+ channel blocker
Amiodarone/ Cordarone
MOA of Amiodarone/ Cordarone
potassium channel blockade
drug that contains high levels of iodine
Amiodarone/ Cordarone
drug that causes Blue-gray coloring of skin can occur as a result of iodine deposition
Amiodarone/ Cordarone
primary Class IV/Ca++ channel blocker
Verapamil/ Calan, Isoptin
MOA of Verapamil/ Calan, Isoptin
calcium channel blockade
initial drug of choice for PSVT
Adenosine/ Adenocard
class of atropine
anti-arrhythmic
indication of atropine
cardiac use is in treatment of bradycardia
MOA of Atropine
anticholinergic agent - atropine is a competitive inhibitor of the muscarinic acetylcholine receptors thus it can be thought of as a parasympatholytic.
cardiac drugs which can be administered via an endotracheal tube (for absorption through the lungs)
Atropine, Lidocaine, and Epinephrine (ALE)
side effects of atropine
Blurred vision, dilated pupils, dry mouth and increased heart rate are usually among the first toxic effects of atropine
antidote for organophsophate poisoning
atropine
uses of atropine
cycloplegic to temporarily paralyze accommodation and as a mydriatic to dilate the pupils, diarrhea to decrease secretions and slow peristalsis, preoperatively to decrease bronchial and salivary secretions
classic symptoms of acute organophosphate poisoning
muscarinic in nature…SLUDGE: salivation, lacrimation, urination, diarrhea, gastric distress, emesis
Toxicity due to atropine results in
decreased secretions; flushed, dry, warm skin, visual changes and delirium with hallucinations…Dry as a bone, red as a beet, hot as a hare, blind as a bat, mad as a hatter.
specific antidote for atropine toxicity or tropane alkaloid toxicity is
physostigmine, a reversible acetylcholinesterase inhibitor.
Which has a longer half life and is now seldom used because of increased risks of toxicity: Digoxin or digitoxin?
Digitoxin…both have very low TI’s though
MOA of Digoxin
Inhibitors the Na+/K+ ATPase pump which serves to increase inward current of sodium followed by a greater influx of calcium. Cardiac contraction is enhanced by the increased concentration of intracellular calcium. Also increases renal perfusion.
drug that may cause characteristic flattening or even inversion of the T wave on EKG.
Digoxin/ Lanoxin
drug where you get blurred vision, double vision, flickering dots or flashes of light, halos may appear around objects
Digitalis