Drugs for FINALS Flashcards
All drugs for finals.
Platelet plug formation
- PLT adherance
- 1a - collagen 123
- 1b - vWF + microfibrils
- 2b/3a - vWF + fibrinogen
- Monolayer, spheres, a and b granules
- ADP (Adenosine DiPhosphate), thromboxane A2 and 5HT
- Aggregation + vasoconstriction
Platelet plug inhibition
PGI2 + NO -inhibtits ADP, thomboxane A2, 5HT
vasoconstriction
Aspirin mechanism
Blocks thromboxane A2 irreversibly
Lasts life of PLT 8-9d
Aspirin COUNCILLING
- GI: nausea, bleeds (prophylactic PPI)
- Bronchospasm - 20% asthmatics
- Children: Reye’s syndrome
- Gout (cant leAp)
- Ototoxic
- Anticoagulants: bleed
- Antidepressants: bleed [SSRI, Venlafaxin SSNRI - inhibit 5HT from PLTs)
- Cytotoxic drugs : low excretion of methotrexate
Thiopyridine mechanism
Irreversibly inhibits Adenosine diphosphate (ADP)
Thiopyridine examples
- Ticlipidine
- Clopidogrel
- Prasugrel
- Ticagrelor
Clopidogrel class + mechanism
Irrevers. inhibits ADP
Prasugrel class + mechanism
Irrevers inhibits ADP
Thiopyridine COUNCILLING
- GI
- Bleeding
- Rash
- Severe hepatic impairment
Glycoprotein 2b/3a inhibitor mechanism
- Abcliximab - monoclonca AB
- Aptifibatise/ tirofiban - inhibitors
Abcliximab class + mechanism
Glycoprotein 2b/3a inhibitor
Monoclonal AB
Aptifibatise class + mechanism
Glycoprotein 2b/3a inhibitor
Tirofiban class + mechanism
Glycoprotein 2b/3a inhibitor
ACEi mechanism
BLOCK AG1 to AG2
AG2 functions;
- mass Vasoconstriction (Gq protein)
- ADH (post. pit)
- Aldosterone (adrenal cortex)
- Sympathetic
- Renal NaCL reabsorption (hence water) + K+ excretion (tubules)
ACEi examples
PRIL
- Ramipril
- Perindopril
- Captopril
- Analapril
- Lisinopril
ACEi indications
- Hypertension (1st line)
- HF
- Renal Hypertension (1st)
ACEi COUNCILLING
- Dry Cough 1/10
- First-dose hypotention (start at night)
- +Diuretics/ RAAS – enhances hypotensive effects
- HYPERkalaemia (CI +K supplements/ drugs)
- Angioedema (stop)/ CI Hx
- GI
- Rash (switch, stop)
- Teratogenic
- Renal impairment (stop if Cr >inc>30%/ eGFR dec>25%)
- CI Renovascular disease
- CI Valvular stenosis
- +Lithium toxicity
- +Ciclosporin ARF
- +NAIDS (reduce efficacy)
ACEi monitoring
When to stop?
BP and U+Es
- 2wks
- Annually
STOP: -Serum Cr >20% -eGFR >15%
ARBs mechanism
BLOCK AG2 receptor
AG2 functions;
- mass Vasoconstriction (Gq protein)
- ADH (post. pit)
- Aldosterone (adrenal cortex)
- Sympathetic
- Renal NaCL reabsorption (hence water) + K+ excretion (tubules)
aka AG2 receptor antagonists
ARBs examples
SARTAN’s
- Losartan
- Candesartan
- Irbesartan
- Telmisartan
- Valsartan
ARBs indications
-2nd line to ACEi
- HF (gold has a b A dvd)
- CKD Hypertension 1st (/ACEi)
ARBs COUNCILLING
- First-dose hypotention (start at night)
- +Diuretics/ RAAS – enhances hypotensive effects
- HYPERkalaemia (CI +K supplements/ drugs)
- Angioedema (stop)/ CI Hx
- GI
- Rash (switch, stop)
- Teratogenic
- Renal impairment (stop if Cr >inc>30%/ eGFR dec>25%)
- CI Renovascular disease
- CI Valvular stenosis
- +Lithium toxicity
- +Digoxin fluctuations (candesartan)
ARBs monitoring
BP and U+Es
- 2wks
- Annually
STOP: -Serum Cr >20% -eGFR >15%
Aldosterone antagonist mechanism -also known as?
BLOCKS Aldosterone receptor
- Na/K pump (DT+CD)
- Epithelial Na channel (ENaCs)
- Secretes K+
- Secretes H+ for Na+ (regulating pH, bicarb)
Stimulated by AG2, Adrenal cortex
aka Potassium sparing diuretics
Aldosterone antag examples
Spironolactone
Eplerenone
Aldosterone antag indications
- HF (gold has aba Dvd)
- Post-MI HF
- Hypertension (step 4. K+ <4.5)
- Ascites (cirrhotic pts develop 2ndary hyperaldosteronism)
- Nephrotic syndrome
- Conn’s syndrome (excess aldosterone and low K+ from adrenal cortex)
Aldosterone antag COUNCILLING
- HYPERkalaemia (low K diet)
- CI K+ >4.5 (hyperK = >5.5)
- Risk: ACEi/ ARBs/ supplements
- CI Addison’s disease
- Renal (anuria) (CI, Cr >220half, >310stop)
- Hepatic failure (CI, stop)
- GI
- Gynaecomastia (spironolactone progesterone effects)
- Menstrual irregularities
Aldosterone antagonist monitoring
4x4wk 3x3m 6m
B blocker mechanism
Block sympathetic B-adrenergic input
- Slowing Nodal Phase 0 -ve chronotrope and Myocardial: -ve inotrope
- Systemic - lower BP
B blocker examples
- Atenolol
- Bisoprolol
- Metoprolol
- Nebivolol
- Carvedilol
B blocker indications
- Carvedilol - HF
- Sotalol (2+3) - 1st Rhythm control
- Atenolol - 1st Rate control, MI, Stable Angina(4th), SVT(3rd)
- Bisoprolol - Stable Angina (4th)
- Metoprolol - Stable Angina (4th)
- Propanolol - Migraine prophyl, Anxiety, Thyrotoxicosis
- Last stage of hypertension
B blocker COUNCILLING
- Bradycardia (CI 2/3HB, sick sinus)
- Hypotension (CI uncontrolled HF)
- GI
- Cold-extreminies (CI Reynauds, PVD)
- Bronchospasm (CI asthma)
- Sleep disturbance, nightmares (water-soluble)
- CI +Verapamil (severe brady)
- +Thiazide (insulin resistance, monitor)
CCB mechanism + types
Inhibit Calcium ‘SLOW’ channels
Dihydropyridine (DHP) = vascular smooth muscle
- Peripheral vasodilation, Low BP, Low afterload
non-DHP = Myocardium and conduction system
- Nodal Phase O (-ve chronotrope)
- Myocyte Phase 2 (-ve inotrope)
DHP CCBs examples
PINEs
- Amlodipine
- Nifedipine
- Felodipine
- Lacidipine
Non-DHP CCBs examples
- Diltiazem
- Verapamil
CCB indications
- Hypertension (DHP: 1st >55/ black: Amlopidine)
- Rate control (nonDHP: Diltiazem>Verapamil)
- Angina 4th (nonDHP: Diltiazem, Verapamil)
- Angina 5th Duo (DHP: Nifedipine mod. release + B-blocker)
- Reynauds (Nifedipine + Diltiazem)
- Cluster prophyl (Verapamil)
CCB COUNCILLING
- Non-DHP: Bradycardia (CI 2/3HB, sick sinus)
- Hypotension (CI uncontrolled HF)
- GI (Verapamil: Constipation)
- Flushing
- Ankle oedema (reduce or +ACEi/ARB)
- Gingival hyperplasia
- CI Non-DHP +B-blocker (severe brady)
- CI +Grapefruit juice
Nitrate mechanism
VASO+VENO dilation: Coronary + prevent spasm
VASO (low afterload) -VENO (low preload)
Nitrate examples
- Glyceryl trinitrate (GTN)
- Isosobide mono/ dinitrate
Nitrate indications
Angina to ACS (acutely or every 12hr)
Tolerance: Every 8hrs
Nitrate COUNCILLING
- Flushing
- Hypotension (CI)
- Headache (cerebral vasodilation)
- CI Cerebral haemorrhage
- Tolerance (take every 8hr)
- Tachycardia (CI)
- CI Containing heart disease
Potassium channel activator mechanism
Vasodilation (opens potassium channels)
- Nicorandil: has nitrate-like venodilation (reducing preload)
Potassium channel activator example
Nicorandil
Potassium channel activator indications
Angina (if failed duotherapy with Ca2+ antag + B blocker)
Potassium channel activator COUNCILLING
- Flushing
- Hypotension (CI HF)
- Headache (cerebral vasodilation)
- CI Pregnancy and breast feeding
- Anal ulceration
Loop diuretic mechanism
Inhibit Na-K-2Cl (NaKCC2) co-transporter in thick ascending loop of Henle
Loop diuretic examples
Frusemide Bumetanide
Loop diuretic indications
- HF (acute IV, chronic PO)
- CKD hypertension/ fluid retention (2ndACEi/ARB)
Loop diuretic COUNSILLING
- HYPOkalaemia
- HYPOtension
- Gout (urea absorption, cant Leap)
- Renal impairment
- Liver impairment
- Elderly (low dose)
- CI Pregnancy
- Ototoxic (frusomide)
Loop diuretic monitoring
- 2wk
- 6m