Pharmacy Care Application Flashcards
(37 cards)
Trends in pharmacotherapeutic management of chronic hypertension
- 1st line therapy are ACE-1/ARB, Thiazide, and Calcium Channel Blocker
- Beta blocker are considered the second line agents for the management of HTN (hypertension) alone
- Alpha blockers are generally used for resistant hypertension (Used more frequently for the management of benign prostate hyperplasia (BPH))
LOL, OLOL, ALOL, ILOL
Chemical Nomenclature: Aryloxypropanolanimes
- Multi-ring structures
Pharmacologic Nomenclature: Beta-adrenergic receptor blockers (beta-blockers)
– MOA: act at B-receptors located invidious organs in the body
B1 Vs B2 receptors
- Catecholamines (norepinephrine) bind to B1 receptor and cause cardia automaticity and conduction velocity (increased heart rate)
– Also release renin which learn to BP elevation
– Likely located on the cardiac muscle but not exclusively - B2 receptor cause relaxation of smooth muscles such as lungs
–Result in peripheral vasodilation
– Skeletal muscle stimulation (tremors)
– Work primarily in the pulmonary tissue and the periphery
Alpha 1-receptor
- Involved in the bronchodilation and vasoconstriction effect
- Some Beta blockers exhibit alpha blocking properties
– Labetalol
– Carvedilol
They are referred to as mixed alpha/beta blockers
B-blocker MOA
- Decrease BP by competitively blocking both B1, and B2 adrenergic receptors
– Result in decreased HR and myocardial contractility - Some block Alpha 1 receptor: Decrease peripheral vasoconstriction (Lower BP)
- Intrinsic sympathomimetic activity (ISA)-CAPP
– Partially stimulate beta receptors while blocking catecholamines
– Do not lower HR to the same degree as other beta blockers
Cardio-Selective Beta Blocker
Target B1 receptors preferentially
- Most become non selective in nature at higher dose
- Cause larger effect on HR
- Have smaller effect on BP
Does not always correlate with what the specific B-blocker are used for
Non Cardio-Selective Beta Blocker
Do not lower HR as much as selective Beta Blockers
- Cause BP to lower more by either alpha-blocking or nitric oxide vasodilation
- Can cause bronchoconstriction
– Avoid patient with a history of asthma
– Used with caution in patient with COPD
Therapeutic Categorization and Indication (Beta Blockers)
Hypertension
- Beta blocker only recommended as 2nd line treatment unless patient has another indication requiring beta blockers:
– Angina pectoris (help increase O2 supply)
– Cardiac arrhythmias (atrial fibrillation)
– Myocardial infarction
– Migraine Prophylaxis
– Heart Failure
– Tremors
Contraindication/Warning(Beta Blockers)
Contraindication
- 2nd and 3rd degree AV block or sick sinus syndrome
- Cardiogenic shock
- Cardiac failure/decompensation
Warning
- Caution in patient with diabetes (mask signs of hypoglycemia except for sweating)
- Use caution with bronchospastic diseases
- Peripheral vascular disease
- CNS depression
- Use in acute decompensated heart failure
ADR
- Bradycardia
- Hypotension
- Fatigue
- Dizziness
- Depression
- Decreased Libido
- Impotence
DDI
- Diltiazem/Verapamil
- Digoxin
- Carvedilol, metoprolol, and propranolol are major substrates of CYP2D6 (Any drug that induce or inhibit 2D6 need to be watched out for)
- Carvedilol and propranolol are inhibitors of p-gp
– Cyclosporine, dabigatran, digoxin, ranolazine - Diabetes medication
Counseling Points
- Do not abruptly discontinue beta blockers after using for extended time
– It can lead to rebound tachycardia (increase HR) - Taper beta blockers slowly to avoid rebound effect
- If symptoms of HF appear (SOB, Dyspnea, Swelling of ankles)
- Masks signs of hypoglycemia (will still have sweating and hunger)
Non-selective individual Compounds
- ‘67 - propranOLOL (Inderal-IV available)
- ‘78 - timOLOL (Blocadren)
- ‘79 - nadOLOL (Corgard)
- ‘82 - pindOLOL (Visken)
Cardio-Selective Beta Blockers
- MetoprOLOL tartrate (Lopressor, Toprol XL)
- AtenOLOL (Tenormin)
- AcebutOLOL (Sectral)
- EsmOLOL (Brevibloc-IV available)
- BetaxOLOL (Kerlone)
- BisoprOLOL (Zebeta)
- NebivOLOL (Bystolic)
Mixed non-selective and Alpha1 blockers
- CarvedILOL (Coreg) most commonly non selective
- LabetALOL (Trandate, Normodyne) commonly used for pregnant women as it is most safe in that regard
Ophthalmic Beta Blocker
- LevobunOLOL (Betagan Liquifilm)
- BetaxOLOL (Betoptic)
- MetiparanOLOL (Optipranolol)
- CarteOLOL (Ocupress)
- TimOLOL Maleate (Timoptic)
- LevobetaxOLOL (Betaken)
Glaucoma is their sole indication
Darone Products
- AmioDARONE Hydrochloride (got two I in it’s structure)
- DroneDARONE Hydrochloride
Amiodarone Indications
Anti-arrhythmic agent used primarily for ventricular arrhythmias:
- Non-sustained ventricular tachycardia (VT)
- Sudden cardiac arrest dur to ventricular fibrillation/pulseless VT
Off Label:
- Pharmacological cardio version in atrial fibrillation (Afib)
- Maintenance of sinus rhythm
- Prevention of post operative atrial arrhythmias
Dose used is dependent on the type of arrhythmias being treated
- Lower doses are generally used for atrial arrhythmias
Amiodarone MOA
- Class III Antiarrhythmic
- Inhibits adrenergic alpha and beta receptors
- Affect sodium, potassium and calcium channels
– Prolongs the action potential and refractory period and decreases AV conduction and sinus node function - Hald life is 40 to 55 days
Amiodarone: Adverse events
Most side effect is seen after an extended period of time
- Affect several systems
– Pulmonar - fibrosis, pneumonitis
– Thyroid - hypo/hyperthyroidism
– Ophthalmic - blurred vision, visual halos
– Gastrointestinal - anorexia, causes, vomiting
– Cardiovascular - hypotension, bradycardia, QT prolongation
– Dermatologic - photosensitivity
– Hepatic - abnormal LFTs
BBW (Amiodarone)
- Hepatotoxicity
- Pulmonary toxicity
- Ability to worsen arrhythmias
- Use should be limited to patient with life threatening arrhythmias
Interactions (Amiodaron)
- Drugs that prolong QTc
- Warfarin
- Substrate: CYP3A4, CYP2C8
- Inhibits: CYP2C9, CYP2D6, CYP3A4 (grapefruit juice)
Availability
Brand Names
- CardarONE
- PacerONE
Got 50 mg/mL IV injection
Dronedarone
- Class III anti arrhythmic agent-indicated to reduce the risk of cardiovascular hospitalization
- For patient with:
– Paroxysmal
– Persistent atrial fibrillation
– Atrial flutter with recent episode - Associated risk factors:
– Age>70
– HTN
– Diabetes
– Prior stroke
– Structurally similar to amiodarone but lack iodine moiety - Only available as 400 mg tablets under brand name MUTAQ
