Drugs in Red Exam 4 Flashcards
(107 cards)
1
Q
Serotonin
A
- 5-HT, Indoleamine
- Endogenous, monoamine neurotransmitter in CNS
- Regulator of smooth muscle function in CV and GI
- Regulates platelet function
2
Q
Isoproterenol
A
- Synthetic catecholamine
- B1/B2 selective
- Bronchodilator and inotrope
- Used for cardiac benefits: mild/transient episodes of heart block that doesn’t need a pacemaker or electric shock, cardiac arrest, cardiac catheterization (B1)
- Also used to bronchospasms during anesthesia (B2)
3
Q
L-DOPA
A
- product from tyrosine hydroxylase
- AKA dihydroxyphenylalanine
- Decarboxylated by aromatic L-amino acid decarboxylase to form dopamine
- Also used in the formation of histamine, GABA, and 5-HT
4
Q
Dopamine (DA)
A
- Stored in vesicles
- Converted to NE by membrane bound dopamine B-hydroxylase
- Ascorbic acid is cofarctor needed in this conversion
- Can’t cross BBB
- IV Infused
- Metabolized by MAO and COMT, about 25% converted to NE
5
Q
Norepinephrine (NE)
A
- Neurotransmitter in most postganglionic SNS neurons
- Stimulates Alpha 1 (vasoconstricts), alpha 2 (feedback inhibition), and beta 1 receptors (increase HR/contractility)
- Increases systolic and diastolic BP
- Ineffective orally, only IV route
- Short duration, rapid metabolism by MAO and COMT in liver and reuptake at the synapse
- Can’t cross BBB
6
Q
Epinephrine (EPI) - Synthesis, Storage, General Effect
A
- Adrenalin
- NE converted to this in chromaffin cells in the adrenal medulla
- Conversion done by PNMT which is induced by corticosteroids
- Cofactor for this conversion is S-adenosylmethionine
- Stored in chromaffin granules for release (endocrine hormone)
- Stimulant of alpha and beta receptors (no specification)
- Causes fight or flight response (know all of beta 1-3 and alpha 1 response in fight or flight)
- Can’t cross BBB
7
Q
Reserpine
A
- Inhibits VMAT transport that brings catecholamines into their vesicles
- This depletes catecholamines stores from their nerve terminals
- Irreversible inhibition
- Requires new vesicles to be synthesizes which can take days to recover
- Newly synthesized catecholamines metabolized by MAO since VMAT blocks their storage (protection)
- Depletes NE, DA, and 5-HT
8
Q
Tyramine
A
- Indirect acting sympathomimetic
- Taken up by uptake transporters and indirectly release NE
- Compete for vesicular uptake which displaces stored NE
- Makes a carrier available at the inner surface to facilitate exchange diffusion of NE out of vesicle
- No calcium is required, no ATP or DBH is released (nonvesicular release)
- Repeated tyramine administration yields tachyphylaxis - decreased postsynaptic response
- *Need catecholamines to produce their effects**
9
Q
Ephedrine
A
- Indirect acting sympathomimetic
- Also direct acting on B2
- Taken up by uptake transporters and indirectly release NE
- Compete for vesicular uptake which displaces stored NE
- Makes a carrier available at the inner surface to facilitate exchange diffusion of NE out of vesicle
- No hydroxyl groups on ring, can cross BBB
- No calcium is required, no ATP or DBH is released (nonvesicular release)
- *Need catecholamines to produce their effects**
10
Q
Tranylcypromine
A
- Parnate
- MAO-A and B inhibitor
- Used to treat depression
- MAO-A prefers 5-HT and NE
- Irreversible inhibition
- Also used to treat hypertension
- WARNING: “Wine and Cheese Effect” MAO metabolizes tyramine from diet, when blocked if excess tyramine is ingested hypertensive crisis can occur due to tyramine releasing NE
11
Q
Selegiline
A
-Eldepry
-MAO-B inhibitor
-Used to treat Parkinson’s disease
-MAO-B prefers dopamine
-Irreversible inhibition
Also used to treat hypertension
-WARNING: “Wine and Cheese Effect” MAO metabolizes tyramine from diet, when blocked if excess tyramine is ingested hypertensive crisis can occur due to tyramine releasing NE
12
Q
Tolcapone
A
- Tasmar
- COMT Inhibitor
- Adjunct therapies for Parkinson’s disease to prevent dopamine metabolization
- Can possible help reduce the dose of L-DOPA administered
- Act mainly in liver, kidney, and BBB
- Little effect on endogenous catecholamines at synapse
13
Q
Entacapone
A
- Comtan
- COMT Inhibitor
- Adjunct therapies for Parkinson’s disease to prevent dopamine metabolization
- Can possible help reduce the dose of L-DOPA administered
- Act mainly in liver, kidney, and BBB
- Little effect on endogenous catecholamines at synapse
14
Q
Dobutamine
A
- Beta 1 agonist
- Dobutrex
- Increases contractility and chronotropic effects - increase CO
- Only elevates systolic BP
- Diastolic BP and mean arterial pressure are unchanged
- No effect on DA receptors
- IV Infused
15
Q
Metoprolol
A
- Lopressor
- Beta 1 antagonists, competitive
- Used for acute MI (IV), hypertension, angina, and migraine prophylaxis, cardiac arrhythmias related to rapid HR and conduction problems
- Used in cardiology in mild to severe CHF (start at low dose and titrate up)
- Combine with Bisoprolol and Carvedilol to improve injection fraction, slow heart failure, decrease number of deaths/hospitalizations
16
Q
Terbutaline
A
- Brethaire
- Short-acting Beta 2 agonist
- Tablet or parenterally (S.C)
- Used to reverse acute bronchospasm in asthma and COPD
- Off label use - delay/prolong premature labor, don’t use beyond 48-72 hours since this can cause serious maternal heart problems and death
17
Q
Phenyleprine
A
- Neosynephrine
- Alpha 1 agonist
- Potent vasoconstrictor
- Tablets, liquid, nasal sprays
- Combined use with antihistamine, dextromethorphan, acetaminophen
- Metabolized by MAO in liver and intestine
- Therapeutic uses: Nasal congestion in cough, cold, and allergy medications
18
Q
Prazosin
A
- Minipress
- Selective Alpha 1 antagonists
- Reduces BP supine or standing, effects diastolic more
- Used to treat hypertension, hypertensive emergency, Raynaud’s disease, frostbite
- Side effect: syncope with first dose, enhanced vasodilation when given with PDE-5 inhibitors
19
Q
Clonidine
A
- Catapres
- Alpha 2 agonist
- Major side effect is sedation
- Impaired the response to acute glucose challenge in mildly hypertensive, type II diabetic patients
- Doesn’t adversely affect diabetic control over 10 weeks
- Epidural, oral, patch
- ER: Kapvay; Used for ADHD
- Can be used monotherapy or as an add-on for ADHD
- Withdrawal: rebound hypertension
20
Q
Yohimbine
A
- Alpha 2 antagonists
- Effective drug in patients with type II diabetes who have a variant gene ADRA2A
- About 40% of type II diabetic patients have this gene which makes insulin-releasing cells in the pancreas more sensitive to inhibitory effects on insulin release by the stress hormone adrenaline
- New therapeutic option for this subset of people
21
Q
Alpha-methyldopa
A
- Aldomet
- Oral, parenteral
- Treats moderate to severe hypertension
- Forms a false transmitter that displaces NE in synaptic vesicles
- Decarboxylated to methyl dopamine and hydroxylated to methylNE
- Therapeutic antihypertensive effects by activating alpha-2 receptors in CNS
- Black Box Warning: Methyldopa + HCZ - not indicated for initial hypertension therapy
22
Q
Carbidopa
A
- Lodosyn
- Derivative of methyldopa
- Inhibits aromatic amino acid decarboxylase
- Doesn’t cross BBB
- No major effect on endogenous catecholamine synthesis within neuron (effects non-rate limiting step)
- Inhibits conversion of exogenous L-DOPA to dopamine outside of brain which occurs mainly in the liver
- Used in combination with L-DOPA to treat Parkinson’s
23
Q
Guanethidine
A
- Ismellin
- Doesn’t enter CNS
- Taken up by NE neurons and depletes NE stores
- Prevents release of NE in response to action potentials/indirect acting sympathomimetics
- General reduction in sympathetic tone which can treat moderate to severe hypertension
24
Q
Bretylium
A
- Acts like guanethidine
- IV injection
- Used in emergencies to treat ventricular arrhythmias
25
Amphetamine
- Rapid release of neurotransmitter that produces sympathomimetic effect
- Has no hydroxyl groups on ring so it can cross BBB
- Taken up by catecholamine uptake pump in exchange for cytoplasmic catecholamines
- Competes with and displaces endogenous catecholamines
* *Need catecholamines to produce their effects**
26
Amantadine
- Antiviral drug
- Promotes release of dopamine in brain
- Used in treatment of Parkinson's
27
Cocaine
- CII
- Eurphoria and high abuse potential
- Prevents catecholamine reuptake by inhibiting uptake 1 pump
- Indirect sympathomimetic
- Drug of abuse
- High affinity for dopamine uptake pump
- Inhibits reuptake of NE, DA, and 5-HT
- Generalized sympathomimetic effect - Increased HR/BP
- Used as a local anesthetic on mucous membranes of oral, laryngeal, and nasal cavities
- Vasoconstrictor action from NE blockade to decrease bleeding
28
TCAs
- Tricyclic antidepressants
- Ex: amitriptyline
- Prevents catecholamine reuptake by uptake 1 pump
- Act on NE pump > 5-HT pump > DA pump
- No abuse potential
- Takes 2-3 weeks before antidepressant effects are apparent
29
Metoclopromide
- Reglan
- Dopamine D2 antagonist
- Blocks the dopamine inhibition of cholinergic activity
- Increases tone of lower esophageal sphincter
- Increases force of contraction
- Increases gastric emptying
- Effective antiemetic
30
Mirabegron
- Myrbetriq
- Beta 3 agonist
- Relaxation of detrusor muscle to help with urinary incontinence
- Adverse reaction: hypertension
- Combine with antimuscarinic if symptoms persist
31
Prostaglandins & Oxytocin
-Induce labor
32
Prostaglandins/Progesterone Antagonists
-Induce abortions
33
Apraclonidine
- Iopidine
- Opthalmic solution
- Alpha 2 selective agonist
- Decreases aqueous secretions
- Decreased CV side effects
- Similar uses to brimonidine but has a shorter duration
34
Betaxolol
- Betoptic S
- Selective beta 1 antagonist
- Decrease aqueous humor production from ciliary epithelium
- Minimal pulmonary/CV side effects
35
Timolol (Ophthalmic)
- Betimol
- Ophthalmic solution
- non-selective beta antagonist
- Decrease aqueous humor production from ciliary epithelium
- Caution use in those with pulmonary/CV problems
36
EPI PK
- Injection, inhalation, intranasal, or topical to eye
- Not effective orally - metabolized by liver
- Slow IV injection during CPR
- Emergency use
- Loses potency after expiration date due to tendency to auto-oxidize (turns pink/brown)
37
Ana-Kit
- Given SC, IM, or IV
- Given in bronchospasm, severe asthma exacerbation, and anaphylaxis (EPIPEN)
- Beta-2 activation therapeutic use of EPI
38
Racepinephrine
- Asthmanefrin
- OTC inhaler
- Temporary relief of mild symptoms of intermittent asthma
- Beta-2 activation therapeutic use of EPI
39
Vasopressin
- Used along with epinephrine and electrical defibrillation in CPR
- Constricts blood vessels to increase BP
- Alpha 1 effect (via EPI) and V1 receptor (via vasopressin)
- Increases cerebral and myocardial blood flow during CPR
40
Amiodarone/Lidocaine
- Antiarrhythmic drugs
| - Used in CPR
41
Local Anesthetics
- Slows down absorption of anesthetic from site of injection, prolonging its effect
- Used with epinephrine (vasoconstricts via alpha 1 receptor) to treat or prevent surgical bleeding
- Decreases system toxicity
42
EPI Contraindications (5)
1. Use with caution in those with hemorrhagic shock, cardiac disease with coronary insufficiency, cardiac arrhythmias
- Detrimental to above conditions since EPI increases myocardial oxygen demand, increases HR, has proarrhythmic potential, and produces vasoconstriction
2. Hypertension (alpha and beta effects)
3. Hyperthyroidism (B1)
4. Diabetes mellitus (hyperglycemia from B2 activation)
5. Cerebrovascular disease - alpha 1 activation may cause cerebrovascular hemorrhage
43
EPI Adverse Reactions (4)
1. Tissue necrosis from IV leakage, due to alpha constriction of blood vessels (Occurs more at extremities)
2. Anxiety, N/V
3. Cardiac arrhythmias - sinus tachycardias, palpitations, and hypertension
4. Angina - from increased workload and oxygen demands on the heart, occurs in predisposed patients more often
44
Phentolamine
- Regitine
- Alpha receptor antagonist, competitive reversible
- Injected locally to reverse tissue necrosis effect of EPI
- Give ASAP with saline solution once extravasation is noticed
- Given with propranolol to block hypertension from excess catecholamine release before and during pheochromocytoma surgery
- Used in catecholamine-related hypertensive emergencies (cocaine, ampehtamine, clonidine withdrawal, MAO, pheochromocytoma
45
Levophed
- Injectable
- NE product
- Only available as levorotatory isomer
Uses
1. Acute hypotension - non-volume related, used if systolic BP < 70 mmHg
2. Cardiogenic or Septic Shock - use NE, antibiotic therapy, vasopressin, and antibiotics
3. Upper GI Bleeding - administer intraperitoneally or via a nasogastric tube
46
NE Contraindications (3)
1. Hypovolemic - correct volume first
2. Mesenteric Thrombosis - increases risk of ishemia which extends area of infarction
3. Preexisting hyperthyroidism (B1) or hypertension (Alpha1)
47
NE Adverse Reaction (4)
1. Anxiety, N/V
2. CV
3. Tissue necrosis at site of injection
4. Large or repeated doses causes damage to arterial walls and myocardium by forming necrotic areas. Similar lesions occur in patients with pheochromocytoma (occurs in large/repeated doses of EPI/DA too)
48
Quinone
-Causes damage to arterial walls and myocardium from its formation
49
DA Uses (3)
1. Decreases CO, BP, and urinary output in those with septic shock, cardiogenic shock, or post-surgical myocardial failure
* *Gradually D/C to minimize hypotensive response**
2. Treats hypotension
3. Stimulates urine output
50
DA Contraindications (3)
1. Pheochromocytoma
2. Uncorrected ventricular fibrillation, ventricular tachycardia, or other tachyarrhythmias
3. Cardiac disease - increased myocardial oxygen demand
51
DA Adverse Reactions (5)
1. Premature Ventricular Contractions - beta stimulation of myocardium
2. Peripheral vasoconstriction and hypertension from alpha stimulation at high doses
3. Hypotension from D/C abruptly
4. N/V by DA action at CTZ
5. Tissue necrosis
52
Fenoldopam
- Carlopam
- D1 selective agonist
- Short term treatment of severe hypertension
- Dose-dependent blood pressure reduction
- Increases renal plasma flow that stimulates diuresis and natriuresis
- May cause reflex tachycardia
53
MAOI/COMTI
-Potentiate the actions of catecholamines by inhibiting their metabolism
54
TCA/Cocaine/Amphetamine
-Potentiate NE and DA effects by blocking NE uptake pump
55
Alpha/Beta/DA Blockers
-Interfere with postsynaptic response of catecholamines
56
Dobutamine - Uses, Contraindication, Adverse Effects (3)
1. Short-term IV inotropic treatment for decompensated CHF and after cardiac surgery
* *Desensitization with prolonged use**
Contraindications - Hypertrophic subaortic stenosis
Adverse Effects
1. Angina, palpitations
2. N/V
3. Hypertension - increased systolic from increased CO
57
Albuterol
- Proventil, Ventolin
- Short-acting beta 2 agonists
- Inhalation, tablet, solution
- Used in acute bronchospasm in asthma and break through asthmatic symptoms
58
Metaproterenol
- Alupent
- Aerosol inhalation
- Used for acute bronchospasm in asthma and treatment of COPD
59
Levalbuterol
- Xopenex
- R-isomer of Albuterol (S-isomer has no effect)
- Used to prevent bronchospasm in patient 6 or older with reversible obstructive airway disease
60
Salmeterol + Uses (3)
- Serevent
- Long acting B2 agonist
Uses
1. Maintenance/prevention of asthma, use with corticosteroid
2. Bronchospasm prophylaxis for COPD
3. Prevent exercise-induced bronchospasm
61
Advair
- Diskus or HFA
- Fluticasone and Salmeterol
- Maintenance treatment of patients with asthma or COPD
62
Clenbuterol
- Oral long-acting B2 agonist
- Vet use only
- Increases lean body mass by activating beta receptors (B3?)
- Doping substance by most athletic organizations
63
Formoterol
- Foridil
- Long-acting B2 agonist
- Quicker onset than Salmeterol with similar 12 hour duration
64
Long Acting B2 Info/Black Box Warning
- NOT indicated for acute asthma attack of status asthmaticus
- Don't take extra doses when having breakthrough asthma systems
- Not a replacement for corticosteroids
- Step Down therapy to D/C
Black Box Warning
1. Increases risk of asthma-related deaths and hostpitalizations
2. Do not use without using with an inhaled corticosteroid
3. Recommend combination products for pediatric or adolescent patients to increase their adherence
65
Midodrine
- Proamatine
- Oral
- Used for severe postural hypotension
- Avoid near bedtime due to supine hypertension
- Contraindications: severe heart disease, acute renal disease, urinary retention, persistent supine HTN
- Black Box Warning: Marked elevation of supine BP
* *Use in those who can't tolerate fludrocortisone or where non-drug measures fail**
66
Clonidine Uses
1. Treatment of hypertension
2. Withdrawal from opiates, ethanol, and nicotine by blocking sympathetic outflow
3. Treatment of severe pain when given epidurally (Duraclon)
4. Treatment of ADHD, especially with sleep disturbances (ER, good alternative for those who don't tolerate stimulants)
5. Treat anxiety if SNS related
67
Guanfacine
- Intuniv
- Selective alpha 2 agonist, more selective than clonidine
- Treats moderate to severe hypertension
- Also used for ADHD
- Can be monotherapy or add-on
- Good alternative for those who don't tolerate stimulants
- Withdrawal: rebound hypertension, less frequent and severe than clonidine
68
Dexmedetomidine
- Precedex
- Alpha 2 agonist
- Causes sedation and decreased anxiety
- Sedate intubated/ventilated patients in the ICU and non-intubated patients before/during surgeries
- Inhibits SNS, decreases opioid use, doesn't produce respiratory depression
- Half life - 0.5-2.5 hours
- No incidence of rebound tachycardia or hypertension upon withdrawal
69
Brimonidine
- Alphagan
- Opthalmic Solution
- Treats increased IOP from open angle glaucoma or ocular hypertension
- Decreases aqueous humor production and increases outflow through the UVEOSCLERAL pathway
- 1000-fold more selective for alpha 2 than alpha 1 (Alpha1 makes IOP greater and worsens condition)
70
Combigan
-Brimodine and Timolol combination
71
Tizanidine
- Zanaflex
- Muscle relaxant
- Alpha 2 agonist
- Decreases spasticity from MS or spinal cord injuries
- Presynaptic alpha 2 receptors inhibit glutamate release that acts as the neurotransmitter in the corticospinal motor neurons
72
Tramadol
- Ultram
- Alpha 2 agonist
- Affinity for mu - 30%
- Blocks NE receptors - 70%
- Increase NE at synapse, activates alpha 2 receptors
- Inhibits calcium uptake into presynaptic neuron and reduces glutamate release which decreases neurotransmission in pain pathway
73
Amphetamines
- CII
- Amphetamine, Dextroamphetamine, Methamphetamine
- Non-catecholamine sympathomimetic agents
- Stimulates release of catecholamines from vesicles and inhibits their reuptake
- Affects NE and DA in CNS and PNS
74
Adderall
- Equivalent amounts of mixed salts of amphetamine in combination
- XR: once daily
- Black Box: High potential for abuse that may cause sudden death and serious CV adverse reactions
75
Amphetamine Uses (3)
1. ADHD - may make tics worse
2. Short-term obesity treatment (3-6 weeks, then tolerance sets in)
3. Narcolepsy
76
Lisdexamfetamine
- Vyvanse
- Prodrug of dextroamphetamine and l-lysine
- Hydrolyzes in intestine or first pass metabolism
- Limits abuse potential
- Used in ADHD and moderate-severe binge eating disorder
77
Methamphetamine
- Desoxyn, Methampex
- CII
- Used in ADHD and exogenous obesity short-term for those where obesity is refractory to alternative therapy
- Black Box Warning - high potential for abuse, may cause sudden death and serious CV events. Those using it for weight loss should only use if other therapies have been ineffective
78
Methylphenidate
- Ritalin, Concerta, Daytrana
- Dexmethylphenidate - Focalin
- d-enantiomer of methylphenidate (more active)
- CII
- Milder peripheral actions
- Used for ADHD, Narcolepsy, and depression or post-stroke depression when refractory to other therapies
- Numerous sustained release preps available
79
Phentermine
- Adipex-D
- Stimlant
- CIV
- Oral
- Increases NE and DA release and inhibits their reuptake
- Used in short-term obesity treatment adjunct to behavior/diet modifications and exercise
- BMI > 30 or >27 in those with other risk factors
80
Diethylpropion
- Tenuate
- Similar mechanism to amphetamine
- CIV
- Oral
- Manages exogenous obesity in those with BMI or 30 or greater who don't respond to other therapies
81
Ephedrine Uses (4)
1. Acute bronchospasm (beta 2)
2. Hypotension during spinal anesthesia or overdose from hypotensive causing drugs
3. Orthostatic hypotension
4. Nasal congestion
82
Pseudoephedrine
- Sudafed
- OTC
- Oral
- Indirect effect and direct effect on alpha
- Treats nasal congestion and prophylaxis for otitic barotrauma
- Combat Methamphetamine Epidemic Act of 2005 limited amounts purchased
83
Nexafed
- New pseudoephedrine tablet to burn meth production
| - Turns into thick gel when dissolved to make pseudoephedrine harder to extract
84
Modafinil
- Provigil
- CIV
- CNS Stimulant
- Minimal peripheral SE, no tolerance, low abuse
- Improves wakefulness without causing aggression
- Used in Narcolepsy, obstructive sleep apnea, and shift work disorder
85
Atomoxetine
- Strattera
- Treats ADHD in adults and children by selectively blocking NE reuptake
- Doesn't worsen tics
- SE: Decreased appetite
- Lacks abuse potential - good for those with substance abuse disorders
86
Propranolol
- Non-selective beta blocker
- Prototype
- Only l-isomer has adrenergic activity
- Decreases HR, contractility, and renin release
- Decreases bronchodilation as a side effect
- Highly susceptible to first pass metabolism
- Lipophilic, crosses BBB, placenta, and break milk
- Sustained release: 24 hour duration
* *10 USES, ON STUDY GUIDE**
87
Diltiazem
- Cardizem
- Calcium channel blocker
- Can be used in Thyrotoxicosis if beta blocker cannot be used
88
D-Propranolol
-Inhibits the conversion of T4 to T3
89
Nadolol
- Nonselective beta blocker
- Oral
- NOT metabolized by liver, safer to use in patients with liver disease than most other beta blockers
- Used in migraine prophylaxis, anxiety, hypertension, angina pectoris, and antiarrhythmic
90
Timolol
- Blocadren
- Oral
- Nonselective beta blocker
- Used in hypertension, post-MI, angina, migraine prophylaxis
91
Carteolol
- Oral
- Nonselective beta antagonist
- Partial agonists
- Less of an effect than other beta blockers since it has intrinsic sympathomimetic activity
- Treats hypertension and angina
- Minimal bradycardia and disruption of carb metabolism from intrinsic activity
- Good to use in those with diabetes
92
Sotalol
- Betapace
- Nonselective beta blockers
- Antiarrhythmic agent
- Beta blocks and blocks the rapid outward potassium current
- Beta blocker: suppresses extopic beats, reduces myocardial O2 demand, long-term therapy
- Racemix mixture of d and l isomers, act similarly on potassium current
- L-sotalol shown to have beta blocker effects
- Contraindication: asthma
93
Sotalol Warning
- Life threatening proarrhythmia
| - Can cause ventricular tachycardia associated with QT interval prolongation
94
Atenolol
- Tenormin
- Same uses as metoprolol
- Selective beta 1 antagonists
95
Acebutolol
- Sectral
- Oral
- Beta 1 selective antagonist
- Mild intrinsic sympathomimetic activity
- Used for hypertension and ventricular arrhythmias
- Less likely to cause bradycardia
96
Betaxolol
- Kerlone
- Oral and ophthalmic
- Beta 1 selective antagonists
- Minimal systemic absorption via ophthalmic use
- Used for hypertension, chronic open-angle glaucoma, ocular hypertension
- MOST selective beta blocker
- Preferred agents with bronchospastic pulmonary disease
97
Esmolol
- Brevibloc
- Short-acting beta 1 selective
- Continuous IV
- Rapid onset with short duration
- Good when you want beta blocker effects for a short time period
- Used for short-term supraventricular tachyarrhythmias, peri/postoperative HTH or ER hypertensive, acute MI, unstable angina
98
Ivabradine
- Corlanor
- Blocks If heart automaticity channel
- Slows heart rate
- For those with stable HR and CHF
- NOT a replacement for beta blockers or drugs that reduce mortality
- Not recommended for those with arrhythmias
99
Labetalol
- Trandate
- Nonselective beta antagonist, alpha 1 antagonist properties
- Beta to alpha block: 5:1
- Decreases HR, contractility and total peripheral resistance
- Treats hypertension, hypertensive emergency, perioperative hypertension
100
Carvedilol
- Coreg
- Selective beta 1 antagonist, alpha 1 antagonist properties
- Beta to alpha block: 10:1
- Blocks calcium entry to smooth muscle of blood vessels
- Antioxidant effects
- Used for hypertension, angina, protection after acute MY, and to treat mild-moderate HF
101
Nebivolol
- Bystolic
- Seletive beta 1 antagonists and beta 2 agonist properties
- Generates nitric oxide - vasodilation
- B2 effects also vasodilate
- Used to treat hypertension by decreasing HR, myocardial contractility, tone of sympathetic outflow, and renin acitivty
- Additional effect: vasodilation and decreased peripheral vascular resistance
102
Phenoxybenzamine
- Dibenzyline
- Noncompetitive, irreversible alpha 1 and 2 agonist
- Effects last up to 7 days
- Used to treat hypertension with pheochromocytoma, peropheral vasospastic disorders, BPH
103
Tamsulosin
- Flomax
- Selective alpha 1 antagonist for prostate
- Mediates human prostate contraction
- 10x more effective on 1A than 1B receptors on vascular smooth muscle, may not be clinically significant
- Less effect on BP theoretically
- Rapid relaxation of smooth muscle in bladder neck and prostatic urethra
- Doesn't effect size of prostate, can use with 5alpha-reductase inhibitors
- Treats BPH
- May cause retrograde ejaculation
104
Alfuzosin
- Xatral
- Selective alpha 1 antagonist for prostate
- Mediates human prostate contraction
- 10x more effective on 1A than 1B receptors on vascular smooth muscle, may not be clinically significant
- Less effect on BP theoretically
- May be superior for BPH, has no significant side effects on dizziness, asthenia, and ejaculatory dysfunction
105
Finasteride
- Propecia, Proscar
- 5alpha-reductase inhibitor
- Blocks catalysis of testosterone to DHT
- Need to control it to reduce the size of prostate in BPH
- Takes months to work
106
Dutasteride
- Avodart
- 5alpha-reductase inhibitor
- Blocks catalysis of testosterone to DHT
- Need to control it to reduce the size of prostate in BPH
- Takes months to work
107
Jalyn
- Combination of Dutasteride and Tamsulosin
| - Additive effects of 5alpha reductase inhibitor and alpha 1A antagonists to treat BPH
