Adrenergic Drugs Flashcards
1
Q
name the inhibitors of catecholamine storage
A
- amphetamine
- pseudoephedrine
2
Q
amphetamine
A
inhibitor of catecholamine storage
- moa
- releases NE and dopamine (DA) from nerve terminals
- block reuptake of NE by blocking NE transporters
- overall increase of NE levels in synaptic cleft in sympathetic NS and in CNS
- clinical use
- treatment of ADHD
- side effect
- drug abuse
- increased DA in brain = paranoia + hallucinations
3
Q
pseudoephedrine
A
inhibitor of catecholamine storage
- moa
- releases stored NE from nerve terminals
- α and β agonist activity
- clinical use
- treatment of nasal and sinus congestion
- side effect
- CNS stimulation
4
Q
name inhibitors of catecholamine reuptake
A
- cocaine
- imipramine
5
Q
cocaine
A
inhibitor of catecholamine reuptake
- moa
- inhibits NE transporter
- clinical use
- previous use = local anesthetic
- side effect
- drug abuse
- leads to depletion of dopamine which triggers cravings
6
Q
imipramine
A
inhibitor of catecholamine reuptake
- moa
- blocks NE transporter
- clinical use
- treats mild depression
- side effect
- postural hypotension
- tachycardia
7
Q
iproniazid (discontinued now)
A
inhibitor of catecholamine metabolism
- moa
- blocks metabolism of NE in the nerve terminals
- MAOIs increase NE levels which provide more NE available for release into synaptic cleft
- clinical use
- treats depression
- side effect
- must not eat food containing tyramine (fermented foods) since is causes release of NE from nerve terminals
- can cause massive vasoconstriction leading to “hypertensive crisis” which can result in a stroke
- must not eat food containing tyramine (fermented foods) since is causes release of NE from nerve terminals
8
Q
name the α agonists
A
- oxymetazoline
- α1 and α2 agonist
- phenylephrine
- α1 agonist
- clonidine
- α2 agonist
9
Q
describe the moa of α agonists
A
- causes vasoconstriction that increases the total peripheral resistance and increases BP
- no effect on heart but due to causing an increased BP will cause reflex bradycardia
10
Q
clinical usage of oxymetazoline
A
- nasal decongestant (relief due to nasal vasoconstriction)
- ophthalmic hyperemia (vasoconstriction of the conjunctiva)
- eye drops relieve redness and itchy eyes
11
Q
clinical usage of phenyleprhine
A
α1 agonist
- emergency treatment of shock
- nasal decongestant (relief due to vasoconstrictor effect on nasal mucosa
- side effect: hypertension
12
Q
clinical usage of clonidine
A
α2 agonist
- treatment of hypertension
- use in treatment of symptoms associated with drug withdrawal
13
Q
name the β blockers
A
- propranolol
- non-selective β blocker
- atenolol
- selective β1-blocker
- pindolol
- partial β1 agonist
- reduces the effect of endogenous NE at β1 receptors
- partial β1 agonist
14
Q
name the function of β blockers
A
- all β blockers are competitive antagonists
- decreases HR and CO
- decrease SA and AV nodal activity
15
Q
clinical usage and side effects of propranolol
A
- clinical use
- treatment for hypertension and angina
- side effect
- non-competitive, thus more severe sedation, bronchodilation and dyspnea
- bronchoconstriction (COPD + ashtma patients)
- metabolic disturbances (diabetes patients)
- due to decreased glycogenolysis and glucagon secretion
16
Q
clinical use and side effects of atenolol
A
selective β1-blocker
- clinical use
- treatment for hypertension and angina
- reduces blood voluma via decreased renin production
17
Q
clinical usage and side effects of pindolol
A
partial β1 agonist
- treatment for hypertension in patients with bradycardia or low cardiac reserve
- side effects:
- bronchoconstriction
- metabolic disturbances
- partial agonists are weak antagonists, thus weak stimulatory effects on both β1 and β2 receptors
18
Q
name α antagonists
A
- phenoxybenzamine
- α1 and α2 antagonist
- irreversible and non-competitive
- phentolamine
- α1 and α2 antagonist
- reversible and competitive antagonist of NE/Epi
- tamsulosin
- α1 antagonist
19
Q
what is the moa of α antagonists
A
- prevent sympathetically mediated vasoconstriction and hence cause vasodilation and profound fall in BP
20
Q
name clinical use and side effects of phenoxybenzamine
A
α1 and α2 antagonist
- given prior to removal of tumor surgically as to avoid hypertensive crisis
- given for long-term management of pheochromocytoma where surgery not an obvious option
- side effect:
- postural hypotension
- nasal congestion
- failure of ejaculation
21
Q
describe clinical use of phentolamine
A
- treatment of pheochromocytoma
- preferable to phenoxybenzamine since it is reversible
22
Q
name clinical use and side effect of tamsulosin
A
α1 antagonist
- used to treat benign prostatic hyperplasia
- relaxes internal sphincter (trigone muscle) of bladder and relaxes smooth muscle associated with prostate gland which relieves urinary hesitancy
- α1A subtype of the α receptor preferentially expressed in genitourinary smooth muscle
- side effect: postural hypotension, nasal congestion, less reflex tachycardia
23
Q
name clinical use and side effect of prazosin
A
- used to reduce blood pressure
- side effects: marked postural hypotension (particularly after first dose)
24
Q
name the β agonists
A
- dobutamine
- β1 agonist
- albuterol
- β2 agonist
25
name moa, clinical use and side effects of dobutamine
β1 agonist
* moa
* increase HR and force of contraction, thus increasing CO
* clinical use
* used in acute management of heart failure (NOT chronic heart failure)
* side effect
* not usually used for treatment of chronic heart failure since they also increase HR, which makes the heart work harder
26
name the moa, clinical use and side effects of albuterol
β2 agonist
* moa
* powerful bronchodilator effect due to relaxation of bronchial smooth muscle
* clinical use
* used for treatment of asthma
* side effect
* restlessness, anxiety
* tachycardia with high doses due to stimulation of β1
