Drugs Week 6-11 Flashcards
Which drug categories are considered ANTIHYPERTENSIVES? (7)(8)
- Diuretics
- Calcium Channel Blockers
- Beta Blockers
- ACEi Inhibitors
- ARB
- (Direct Renin Inhibitor)
- Central Acting Alpha Agonist
- Nitrates
What are diuretics used for?
-Limit water and sodium reabsorption, this causes increased excretion of NA+ and water by kidneys.
What is the recommended initial therapy for all HTN patients?
Diuretics
What are the three main classifications of diuretics?
Short explanation of each.
Loop diuretics:
- acts on ascending limb of loop of Henle - inhibits reabsorption of Na/K/2CL, thus preventing reabsorption of water that follows
Thiazide diuretics:
- acts on the early part of the distal convoluted tubes - inhibits mechanisms that favor Na+ reabsorption, resulting in Na and K excretion and reabsorption of Ca+
- Potassium-sparing diuretics
- acts on the late part of the distal convoluted tubes
- inhibits the sodium potassium pump, thus limiting the reabsorption of Na+ and excretion of K+
What is the biggest AE in all diuretics?
Dehydration
What are the other AE besides dehydration associated with Loop Diuretics?
- hypokalemia (K+)
- hyponatremia (Na+)
- hypocalcemia (Ca+)
- ototoxicity (ear)
- hyperglycemia
What is an example of a Loop Diuretic?
furosemide (Lasix)
What are the AE associated with Thiazide Diuretics?
- Same as loop diuretics except:
- hypercalcemia
- significant loss of K+
What is an example of a Thiazide Diuretic?
hydrochlorothiazide (HCTZ)
Why are Thiazide Diuretics helpful for older adults?
Thiazide diuretics reabsorb calcium unlike loop diureteics. This helps maintain bone density and prevent kidney stones.
What is the biggest AE associated with Potassium Sparing Diuretics?
Hyperkalemia
What is an example of a Potassium Sparing Diuretic?
What is different about this drug?
- spiranolactone
- It blocks aldosterone receptors which can produce:
- gynecomastia in males
- menstrual irregularities in females
Which diuretic is the most common?
Which diuretic is less effective in producing diuresis?
- Thiazide
- Potassium Sparing
All diuretics reduce plasma volume. What does this cause?
-hyperglycemia
What drugs counteract diuretics?
NSAIDs (Na+ retention)
What are calcium channel blockers used for?
Block Ca2+ entrance into vascular smooth muscles, thus disallowing excitability, which in return causes vasodilation.
What are the AE assoiated with all calcium channel blockers?
- HA
- dizziness
- hypotension
- bradycardia
- reflex tachycardia
What are the three classes of Ca+ Channel Blockers?
What do they each act on?
Dihydropyridines:
-reduce arteriolar tone
Phenylalkyamines:
-affect the heart
Benzothiazepines:
-affect heart and vasculature
When are Ca+ Channel Blockers useful?
When Beta Blockers are contraindicated.
What is an example of a dihydropyridine?
amlodipine
What is an example of a benzothiazepine?
diltiazem
How do Beta Blockers work?
What does this result in?
Block the effect of (nor)epinephrine. Act as a competitive antagonist of Beta adrenoceptors
Results in negative inotropic effect (SV)
Results in negative chronotropic effet (HR)
What does it mean when a Beta Blocker is nonselective?
It blocks both B1 and B2 adrenoceptors.
If it were selective it would only block B1.
Ultimately, Beta Blockers job is to reduce _________ influences. This in return means a reduce in what?
Sympathetic
Workload of the heart
What is an example of a NONSELECTIVE Beta Blocker drug?
-propranalol
What are the 2 cardioSELECTIVE (B1) Beta Blockers?
- metropolol
- carvedilol
When a patient is on a Beta Blocker, should we monitor exercise tolerance by HR?
No, must use a different rate
What do Beta Blockers usually end in?
“-lol”
How do ACEi drugs work?
They block the conversion of angiotensin I to angiotensin II
angiotensin II acts to constrict blood vessels, ACEi drugs inhibit this
What do ACEi drugs usually end with?
“-pril”
What are the AE associated with ACEi drugs?
Common
- Dry cough
- Hypotension
- Hyperkalemia
Rare, serious AE:
- Acute renal failure
- Angioedema
What patients would be on an ACEi drug for an extended amount of time?
Stroke victims
What are some examples of ACEi drugs?
- lisinopril
- enalapril
- ramipril
How do ARBs work?
Blocks the binding of angiotensin II at AT1 receptor
What are the AE of ARBs?
Same as ACEi but without the dry cough
What do ARBs end in?
“-sartan”
When are ARBs used?
When ACEi intolerant, or when a cough is developed while on ACEi
What are some examples of ARBs?
- losartan
- valsartan
What type of drug is the best tolerated of all HTN medications?
ARBs
What is considered the triply whammy?
ACEi, Diuretic, NSAID
How do Direct Renin Inhibitors work?
Block conversion of angiotensinogen to angiotensin I
What are the AE of Direct Renin Inhibitors?
Similar to ACEi/ARB
Should we take RAAS inhibitors in combination with other drugs?
No, due to increased AE
How do Central-Acting Alpha Agonists work?
Directly act on the CNS presynaptic neurons to cause a negative feedback loop resulting in less norepinephrine production.
What are the AE of Central-Acting Alpha Agonists?
- Dizziness
- Drowsiness
- Fatigue
- HA
What is an example of a Central-Acting Alpha Agonist drug?
What is it reserved for?
AE?
Route?
clonidine
- reserved for resistant HTN
- dry mouth, rash with patch
- PO or weekly patch
How do Nitrates work?
- Work directly on smooth muscle instead of a receptor (MOA unknown)
- Appears to decrease preload and afterload which in return reduces the workload of the heart
What are the forms of nitrate?
Which are long acting and which are short acting?
Long acting:
- oral
- transdermal
Short acting:
- sublingual
- chewable tablet
- IV
What are some examples of nitrates?
- nitroglycerin
- isosorbide mononitrate
What is different about ISMN (isosorbide mononitrate) and ISDN (isosorbide dinitrate)?
ISDN undergoes significant first-pass metabolism and has a half-life of 1 hour.
ISMN has a half-life of 4-6 hours
What is unique about the storage of nitrates?
- Limited light exposure (kept in brown bottle)
- Short shelf life (6m unopened, 3m opened)
- Tingling sensation as drug dissolves= active drug
Dosing of nitrates:
- After 1st dose, relief should occur in ____.
- 2nd dose if symptoms are still present after ___ (up to _ doses in __ minutes)
-1-2 minutes
5 minutes/ 3 doses in 15 minutes
What is possible if no relief occurs?
Possible MI
What are the AE of nitrates?
- reflex tachycardia
- dizziness
- OH
What situations are nitrates used in?
Angina and HTN (adjunct treatment)
What other drugs are used to treat angina?
Beta Blockers and Calcium Channel Blockers
END ANTIHYPERTENSIVE DRUGS
END ANTIHYPERTENSIVE DRUGS
List of need to know ANTITHROMBOTIC drugs.
- Aspirin
- Clopidogrel (Plavix)
- Enoxaparin (Lovenox)
- Apixaban (Eliquis)
- Rivaroxaban (Xarelto)
What are some examples of conditions that would need Antithrombotic drugs?
Venous thrombosis:
- Superficial- UE or LEs, due to varicose veins
- Deep- 3rd most common CV disease
Pulmonary Emboli
- often originate in deep veins of pelvis and legs
- lodges in lung capillaries
Pulmonary emboli can happen ______ ________.
Without warning
What are the three subclasses of antithrombotics?
- Antiplatelets
- Anticoagulants
- Fibrinolytics
L8S26 HEMOSTASIS
L8S26
How do antiplatelets work?
Prevent the aggregation of platelets
How does the Antiplatelet Aspirin work?
- Inhibits COX-1 and COX-2 which decreases the production of thromboxane A2 which inhibits platelet aggregation
- At low doses (81mg), COX-1 is the primary one inhibited for CV protection
How do Antiplatelets- ADP Receptor Inhibitors (Irreversible) work?
- active metabolite irreversibly blocks P2Y12 receptors on platelets
- blocks ATP binding
- blocks activation of GP IIb/IIIa receptor complex
- decreases platelet aggregation
In Short:
- blocks ADP binding
- blocks GP IIb/IIIa
- decreases aggregation
Since these drugs are irreversible, how long will they last after discontinuing the drug?
lifespan of the platelet (7-10 days)
What is an example of a ADP Receptor Inhibiting (Irreversible) Antiplatelet?
clopidogrel (Plavix)
Plavix is a ________ and ________ antagonist
noncompetitive and irreversible
What is the biggest concerns with these drugs?
- Bleed, avoid falls
- DD interactions can impact efficacy of these drugs
What is the difference between a Reversible and Irreversible ADP Receptor Inhibitor?
Reversible can have a shorter impact, most everything else is the same.
When are ADP Receptor Inhibitor Antiplatelets used?
- ACS (acute coronary syndrome)
- stroke= only Plavix
What are the Parenteral Anticoagulants?
What are the PO Anticoagulants?
Parenteral
- Heparin
- Low-molecular weight heparin (LMWH)
- Fondaparinux (Arixtra)
- Direct thrombin inhibitors
PO
- Vitamin K antagonist
- Direct thrombin inhibitor
- Factor XA inhibitors
How does Heparin work?
Potentiates antithrombin which inactivates thrombin and FXa.
This results in the preventing the conversion of fibrinogen to fibrin.
How does LMWH work?
Works like Heparin but has a greater effect on inhibiting FXa than thrombin
Is Heparin or LMWH preferred?
LMWH
What is the most common LMWH?
enoxaparin (Lovenox)
How do IV Direct Thrombin Inhibitors work?
Bind directly and reversibly to thrombin
Which 2 drugs are more specific to factor Xa?
LMWH and fondaparinux (Arixtra)
How does Warfarin (VKA) work?
Binds to KORC1, an enzyme that converts inactive vitamin K to active vitamin K, depletes vitamin K stores, which in return inhibits synthesis of Factors… and protein C and S
What is the reversal agent of Warfarin?
Vitamin K
Does Warfarin have an immediate effect?
No, 3-5 days for full effect. Longer to stabilize dose.
Warfarin is considered a ___ drug, meaning it requires frequent monitoring of INR (normal~1).
NTI
What is considered normal INR for AF and VTE?
2-3
Warfarin has ____ drug and food interactions
many
How do Factor XA inhibitors work?
selectively and reversibly binds to FXa which stops further coagulation cascade
What do factor XA Inhibitors end in?
“-xaban”
What are some examples of XA Inhibitors that are commonly prescribed?
- rivaroxaban (Xarelto)
- apixaban (Eliquis)
What are the main things to monitor for when taking antiplatelets or antithrombotics?
- Bleeding
- Clotting
How do Fibrinolytics work?
Breaks fibrin links in the thrombus
When do we use Fibrinolytics?
After stroke, MI, PE
Fibrinolytics are the only meds that do what?
Break up a clot
What is atherosclerosis?
What kind of LDL and HDL numbers do we want?
-Narrowing and hardening of the arteries
- LDL= want it low
- HDL= want it high
What are the medication used to treat atherosclerosis?
- HMG-CoA Reductase Inhibitors (Statins)
- PCSK9 Inhibitors
- Bile Acid Sequestrants
- Fibrates
- Omega-3 Fatty Acids
- Niacin
How do HMG CoA REDUCTACE INHIBITORS “Statins” work?
Block HMG-CoA reductase= blocks cholesterol synthesis.
What is the most common AE of Statins?
Myalgia
What are other AE of Statins?
- Dyspepsia
- HA
- increase liver function enzymes\
- possible tendon rupture
What are some examples of some Statins?
- Atorvastatin (Lipitor)
- Rosuvastatin (Crestor)
- Simvastatin
- Pravastatin
What are some other cardiac meds that are used?
- sacubitril/valsartan (Entresto) (ARNI class)
- Digoxin
- Amiodarone
Both sacubitril and valsartan act to do what?
Increase vasodilation
How does digoxin work?
- Inhibits Na+/K+ ATPase pump in myocardial cells.
- Helps the heart beat stronger and with a more regular rhythm
What is Digoxin mainly used for?
Symptom control
What is the main S/Sx of toxicity with Digoxin?
Visual changes (halos around yellow-green color spectrum)
Who is mainly at risk for toxicity?
- Low body weight
- Advanced age
What is arrhythmia?
A disturbance of HR or rhythm
What is arrhythmia classified by? (3)
Origin-ventricular or atrial
Pattern- fibrillation or flutter
Speed/rate- brady or tachy
Arrhythmia means there is a dysfunction in the what?
SA node
What is an example of a drug used to treat arrhythmia?
amiodarone
How does amiodarone work?
Prolongs the duration of the action potential by blocking K+ channels.
Used for ventricular arrhythmias
Important AE to note with amiodarone?
- Bluish discoloration on exposed areas of the skin
- LFTs, TFTs, PFTs
Does amiodarone have a short or long half life?
Long (50 days)
INHALED MEDICATIONS are divided into what subclasses?
- Inhaled Beta Agonist Medications
- Inhaled Antimuscarinic (antocholinergic)
- Inhaled Corticosteroids
- Combination Inhaled Medications
- Inhaled Mucolytic
How do Inhaled Beta Agonists work?
Agonize B2 receptor= bronchodilation
What do Inhaled Beta Agonists end in?
“-terol”
Inhaled Beta Agonists are divided into what 2 categories?
SABA
LABA
What is an example of a Inhaled Beta Agonist?
albuterol (ProAir, Ventilon)
How do Inhaled Antimuscarinics work?
Bind M3 in airway smooth muscle; antagonizes ACh actions at these sites= bronchodilation
Inhaled Antimuscarinics are divided into what 2 categories?
SAMA
LAMA
What are the AE of Inhaled Antimuscarinics?
Dry mouth
generally well tolerated
What is an example of a Inhaled Antimuscarinic?
Is it a SAMA or a LAMA?
tiotropium (Spiriva)
Long Acting
What are Inhaled Corticosteroids usually used for?
Exacerbations or more severe disease
What is the main AE of Inhaled Corticosteroids?
oral candidiasis
What do most Inhaled Corticosteroids end in?
“-asone”
What is an example of a Inhaled Corticosteroid?
fluticasone (Flovent)
What is the purpose of Combination Products?
May increase effect with lower AE as compared to increase in dose of a single product
What are some examples of Combination Products?
- fluticasone/salmeterol (ICS/LABA) (Advair)
- formoterol/budesonide (LABA/ICS) (Symbicort)
- albuterol/ipratropium (SABA/SAMA) (Combivent)
How do Inhaled Mucolytics work?
Cleave DNA thus decreasing mucous viscocity which improves airflow
What are the AE of Inhaled Mucolytics?
- chest pain
- cough
- voice disorder
- skin rash
What are some examples of Inhaled Mucolytics?
- hypertonic saline
- dornase alfa (Pulmozyme)
How do Leukotrine Modifiers work?
Release from mast cells and eosinophils to play a role in airway edema
What is an example of a Leukotrine Modifier?
-montelukast (Singulair)
What is montelukast used for?
Asthma
-take once daily in evening (for allergies can only use in the AM)
How do Immunomodulators: Anti IgE work?
binds IgE antibodies which prevents IgE binding to receptors on mast cells and basophils
What are the AE of Immunomodulators?
HA, injection site reaction
What is an example of an Immunomodulator: Anti IgE?
omalizumab (Xolair)