Beta blockers, Alpha blockers and stimulants, direct, emergencies Flashcards Preview

Pharm HTN > Beta blockers, Alpha blockers and stimulants, direct, emergencies > Flashcards

Flashcards in Beta blockers, Alpha blockers and stimulants, direct, emergencies Deck (81):
1

What are the Sympathetic effects of Alpha 1?

- Vasoconstriction
- Increased peripheral resistance
- Increased BP
- Mydriasis (dilate pupils)
- Increased closure of internal sphincter of the bladder

2

What are the Sympathetic effects of Alpha 2?

- Inhibition of norepinephrine release
- Inhibition of acetylcholine release
- Inhibition of insulin release

3

What are the Sympathetic effects of Beta 1?

- Tachycardia
- Increased lipolysis
- Increased myocardial contractility
- Increased release of renin

4

What are the Sympathetic effects of Beta 2?

- Vasodilation
- Slightly decreased peripheral resistance
- Bronchodilation
- Increased muscle and liver glycogenolysis
- Increased release of glucagon
- Relaxed uterine smooth muscle

5

Within the sympathetic system we can affect blood pressure by doing what?

- Blocking the beta-1 receptors

- Blocking peripheral alpha-1 receptors

- Trigger central alpha-2 receptors

6

What does Blocking the beta-1 receptors do?

- Reduce heart rate
- Reduce renin release

7

What does Blocking peripheral alpha-1 receptors do?

- Vasodilation
- Decreased peripheral resistance

8

What does Triggering the central alpha-2 receptors do?

Reduce sympathetic outflow to the heart

9

What are the 3 main Beta Blockers we need to know?

• Carvedilol (CoregTM)
• Metoprolol (LopressorTM, Toprol XL)
• Nebivolol (Bystolic)

10

What is the prescription for Metoprolol Ext. Rel.?

100 mg
One tablet daily

- Max dose = 400 mg

11

What is the prescription for Carvedilol?

12.5 mg
One tablet twice a day

12

What is the prescription for Bystolic™?

20 mg
One tablet daily

- May start at 5 mg and titrate up

13

What are the differences based on for the Beta Blockers?

Selectivity

14

What are the 3 categories of Selectivity for the Beta Blockers?

1.) Non-selective beta-blocker:
- Block both beta-1 and beta-2 receptor sites
- Example: propranolol

2.) Selective beta-blockers
- Specifically block beta-1 receptors
- Example: metoprolol

3.) Beta-blockers with peripheral vasodilatory effects
- Adds in an alpha-1 blockade effect --> Example: labetolol, carvedilol
- Affects nitric oxide levels --> Example: nebivolol

15

What is Atenolol indicated for?

- Treatment of hypertension, alone or in combination with other agents
- Management of angina pectoris
- Secondary prevention postmyocardial infarction

16

What is Carvedilol (Coreg™, Coreg CR™)
indicated for?

 Management of hypertension
 Mild-to-severe heart failure of ischemic or cardiomyopathic origin
 Left ventricular dysfunction following myocardial infarction (clinically stable with LVEF ≤40%)

17

What is Metoprolol succinate (Toprol XL™) indicated for?

 Treatment of hypertension
 Treatment of angina pectoris
 To reduce mortality/hospitalization in patients with heart failure (stable NYHA Class II or III) already receiving ACE inhibitors, diuretics, and/or digoxin

18

What is Nebivolol (Bystolic™) indicated for?

Treatment of hypertension, alone or in combination with other agents

19

What is the candidate for use of Beta Blockers?

Younger patients rather than older patients

20

What is the effectiveness of Beta Blockers?

- No evidence for primary prevention of hypertension
- Preferred agents for patients with cardiac disease

21

What Agents would require dose adjustments in patients with renal impairment?

Atenolol

22

What drugs have Hepatic metabolism and need no renal dose adjustment but have first pass effect issues?

Metoprolol, carvedilol

So oral is higher dose than IV

23

Because of lipid and water solubility and possible penetration of blood brain barrier, Beta Blockers could cause?

Theoretically beta blockers in the CNS would cause effects such as: Lethargy, Nightmares, Confusion, Depression

24

Beta Blockers that are water soluble have?

- Less tissue penetration
- Longer biological half-lives

Ex: atenolol

25

What are the Adverse effects of Beta Blockers?

- Many side effects related to effects on cardiac tissue: Bradycardia, Hypotension, Atrioventricular nodal conduction block
- Bronchoconstriction
- Hypoglycemia

26

What are the Alpha Blockers?

***Doxazosin (Cardura)
- Prazosin (Minipress)
- Terazosin (Hytrin)

27

What is the prescription for Doxazosin?

8 mg
One capsule daily

28

How do the Alpha Blockers work?

o Blockade of alpha-1 receptors
 Affect both arteriolar and venous resistance vessels
• Magnitude based on sympathetic system activity
• Body response to fall in blood pressure can be
o Increase in heart rate
o Increase in cardiac output
o Increased fluid retention

29

What are the Adverse Drug Reactions of the Alpha Blockers?

o Orthostatic hypotension
 Increased fall risk
 Easing into therapy or dose changes (First dose syncope)
o Aggravators
 Nasal congestion, headache, reflex tachycardia, peripheral edema (B/c good at opening up blood vessels)
o Non-selective alpha blockade
 Smooth muscles of the base of the urinary bladder

30

What are the differences between the alpha blockers?

o Biological half life --> Doxazosin has longest half life

31

What is Prazosin (Minipress) indicated for?

Treatment of hypertension

32

What is Terazosin (Hytrin) indicated for?

- Management of mild-to-moderate hypertension; alone or in combination with other agents such as diuretics or beta-blockers
- Benign prostate hyperplasia

33

What is Doxazosin (Cardura) indicated for?

 Treatment of hypertension as monotherapy or in conjunction with diuretics, ACE inhibitors, beta-blockers, or calcium antagonists
 Treatment of urinary outflow obstruction and/or obstructive and irritative symptoms associated with benign prostatic hyperplasia

34

What is a positive effect of the alpha blockers?

- Favorable effect on lipid profile?
- Diminish risk of atherosclerosis by this mechanism and reduction of effect of cathecholamines in stimulation of vascular smooth muscle hypertrophy

35

What are the Alpha Stimulants?

- Clonidine (Catapres™)
- Methyldopa (Aldomet™)
- Guanfacine (Tenex™)
- Guanabenz

36

Prescription for Clonidine?

200 mcg
One tablet twice a day

37

Prescription for Catapres TTS™?

0.2 mg/24 hrs
Apply one patch once every 7 days

38

Prescription for Methyldopa ?

500 mg
One tablet twice a day

 Initial dose is 4 times a day, 2 times a day is maintenance dose
 Mainly used in pregnancy


39

How do the Alpha Stimulants work?

No one knows?
Theory = brain with drug doesn't let vessels clamp down

40

What is the difference between the Alpha Stimulants?

Pharmacokinetics

41

What is Methyldopa indicated for?

Management of moderate-to-severe hypertension

42

What is Clonidine indicated for?

 Management of hypertension (monotherapy or as adjunctive therapy)
 Tablets or patch

- Can be used to treat pain syndrome or heroine addicts going through withdrawal

43

What is Guanfacine indicated for?

- Management of hypertension

- May be used in extended release form to treat ADHD

44

What is Guanabenz indicated for?

Used alone or in combination with other classes of antihypertensive agents in the management of hypertension.


NOT available in US

45

What are the Adverse Drug Reactions of the Alpha Stimulants?

o Dry mouth
o Bradycardia
o Orthostatic hypotension
o Sedation

o Problem with abrupt withdrawal
 Life-threatening hypertensive crisis

46

What are the Direct Vasodilators?

• Minoxidil
• Hydralazine

47

What is the Prescription for Minoxidil?

5 mg
One tablet daily

48

How does Minoxidil work?

 Increase in nitric oxide levels
• Increase in nitric oxide equals vasodilation (both arterial and venous)
• Vasodilation equals drop in blood pressure

49

What are the Adverse Drug Reactions for Minoxidil?

 Standard side effects for an antihypertensive and then…
• Oops!
o Pericarditis and pericardial effusion that could progress to tamponade
o Increase oxygen demand and exacerbate angina
o Some sodium and water retention leading to…
• Grow hair (used in Rogaine)

50

What is the prescription for Hydralazine?

50 mg
One tablet twice a day (maintenance dose)

 Initial dose = 4 times a day

51

How does Hydralazine work?

 Opening up potassium channels in vascular smooth muscle
 Increased nitric oxide levels
 You got me!

- is effective at vasodilating

52

What are the Adverse Drug Reactions for Hydralazine?

 Blood pressure drop significant enough to cause reflex tachycardia
• Give with beta blocker to blunt effect
 Adverse drug reactions
• Headache
• Lupus-like syndrome
o Inflammation, fatigue, more in women

53

What is a Hypertensive Emergency?

o Severe elevations in blood pressure
o Often higher than 220/140 mm Hg
o Requires immediate attention and blood pressure reduction

54

What is a Hypertensive Urgency?

o Marked elevation in blood pressure
o Usually higher than 180/110 mm Hg
o S/S headache, shortness of breath, pedal edema
o Management with oral agents may be appropriate

55

What are the oral agents you can use in an Hypertensive Urgency?

o Captopril
o ***Clonidine
o Labetalol
o Amlodipine

56

What is the Dosage for Captopril?

• 25 mg PO, repeat as needed,
• SL- 25 mg

57

What is the Onset/duration for Captopril?

- PO:15-30 min/6-8 hrs
- SL: 10-20 min/2-6 hrs

58

What are the Adverse Drug Reactions for Captopril?

Hypotension, renal failure, bilateral renal stenosis

59

What is the Dosage for Clonidine?

0.1-0.2 mg PO, repeat hourly as required to total dosage of 0.6 mg

60

What is the Onset/duration for Clonidine?

30-60 min/8-16 hrs

61

What are the Adverse Drug Reactions for Clonidine?

Hypotension, drowsiness, dry mouth

62

What is the Dosage for Labetalol?

200-400 mg PO, repeat every 2-3 hours

63

What is the Onset/duration for Labetalol?

1-2 hr/2-12 hrs

64

What are the Adverse Drug Reactions for Labetalol?

Bronchoconstriction, heart block, orthostatic hypotension

65

What is the Dosage for Amlodipine?

2.5-5 mg PO

66

What is the Onset/duration for Amlodipine?

1-2 hr/12-18 hr

67

What are the Adverse Drug Reactions for Amlodipine?

Tachycardia, hypotension

68

What are some of the major Hypertensive Emergency Injectables?

o Sodium Nitroprusside
o Nitroglycerin
o Nicardipine

69

What is the Dosage for Sodium Nitroprusside?

0.25-10 mcg/kg/min IV infusion

70

What is the Onset/Duration for Sodium Nitroprusside?

Immediate/2-3 min after infusion stop

71

What are the Adverse Drug Reactions for Sodium Nitroprusside?

• TOXIC!!!
• Nausea, vomiting, cyanide poisoning, metabolic acidosis, arrhythmias, death

72

What is the Dosage for Nitroglycerin?

• 5-100 mcg IV infusion

73

What is the Onset/Duration for Nitroglycerin?

2-5 min/5-10 min after infusion stop

74

What are the Adverse Drug Reactions for Nitroglycerin?

Headache, tachycardia

75

What is Sodium Nitroprusside used for in special cases?

• Acute Coronary Syndrome, Heart failure, Acute or Chronic Renal Failure, Ischemic Stroke

76

What is Nitroglycerin used for in special cases?

Acute Coronary Syndrome, Heart failure

77

What is the Dosage for Nicardipine?

5-15 mg/hr IV infusion

78

What is the Onset/Duration for Nicardipine?

1-5 min/15-30 min*

79

What are the Adverse Drug Reactions for Nicardipine?

Tachycardia, nausea, increased intracranial pressure

80

What is Nicardipine used for in special cases?

• Acute Coronary Syndrome, Acute or Chronic Renal Failure, Ischemic Stroke

81

How might you be limited by laws in your state in prescribing meds for hypertensive urgencies or emergencies?

- You may be limited by state laws, regulations, etc., as to the extent of your ability to prescribe injectable vasoactive products
- You are likely not limited by state laws, regulations, etc as to the extent of your ability to prescribe oral vasoactive agents
1. Familiarize yourself with oral options for hypertensive urgencies
2. Know the IV approaches to hypertensive emergencies so you can guide others
3. Be careful!