Sympathomimetic Drugs/ Adrenoceptor Agonist Flashcards
(71 cards)
1
Q
Receptors present in somatic motor neuron terminals
A
Beta 2 adrenergic
2
Q
Which receptors binds only to epinephrine
A
Beta 2 adrenergic receptor
3
Q
Beta 1 location and function
A
Fat cells
Lipolysis
4
Q
D1 location and function
A
Splanchnic and renal blood vessel
Relaxation of vacuolar smooth muscle->Dilation - Dec peripheral vascular resistance
5
Q
D2 receptor
A
On presynaptic nerve terminals
F: inhibits NE, inhibit adenylyl cyclase, open K channels and influx of Ca
6
Q
Beta 3 receptor
A
Lower affinity
Beta 3 resistance to desensitization> beta 1 and 2
7
Q
Epi has increase activity at which receptors
A
Beta 2
8
Q
NE is potent at which receptors
A
Alpha 1 and beta 3
9
Q
Clinical use of phenylephrine and metoxamine
A
- vasoconstrictor
- tx hypotension
- nasal decongestant
- mydrasis
10
Q
Alpha 1 agonist
A
Phenylephrine, Metoxamine ( not cathecol derived- not affected by COMPT)
Milodrine (activated- desglymilodrine)
Xylometazoline
Oxymetazoline( high doses cause hypotension due to clonidiine like effect)
11
Q
Alpha 2 action
A
- on presynaptic terminal - -ve feedback for NE
- ## Hypotension
12
Q
Effect of clonidiine
A
Acts on alpha 2 receptor in brainstem
Hypotension and bradycardia
13
Q
Action of methyldopa
A
- antihypertensive
- high doses stimulate postsynaptic vascular alpha 2 receptor-> vasoconstriction and increase BP
14
Q
Alpha 2 agonist drugs
A
Clonidine Guanabenz Guanfacine Methyldopa Moxonidine
15
Q
If alpha 2 drugs withdrawn to quickly
A
Cause withdrawal symptom’s, and rebound hypertension
16
Q
Tx of orthostatic hypertension
A
Midodrine
17
Q
Side effects of alpha 2 drugs
A
- sedation
- dry mouth
- sleep disturbance
- sexual dysfunctions in males
- nausea
- dizziness
18
Q
Drugs that act on Beta 1 and 2 receptors
A
Isoproterenol
19
Q
Beta 1 selective drug
A
Dobutamin
20
Q
Beta 2 selective drugs
A
Albuterol
Terbutaline
Ritodrine
Metaproterenol
21
Q
Clinical use it epinephrine
A
- tx for anaphylaxis
- use along with anesthetic -> cause vasoconstriction -> Dec absorption-> prolonging anesthetic
22
Q
Mixed alpha and beta agonist
A
- norepinephrine (tx septic shock)
- epinephrine
- phenylpropanolol
- ephedrine
- pseudoephedrine
23
Q
Phenylpropanolamine
A
Mixed adrenergic agonist Vasoconstriction Shrink mucosal surface Otc apatite suppressant Associated with hemorrhagic stroke
24
Q
Phenylpropanolamine
A
Mixed adrenergic agonist Vasoconstriction Shrink mucosal surface Otc apatite suppressant Associated with hemorrhagic stroke
25
Pseudoephedrine
Mixed adrenergic agonist
| Decongestant
26
Use of ephedrine
- asthma therapy
- increase skeletal muscle tone-> M. Gravis
- tx narcolepsy
- nasal decongestant
- promote weight loss
27
Amphetamine like drugs
- amphetamine
- modafinil
- methylphenidate
- phenmetrazine
- tyramine
- methamphetamine
28
Amphetamine roles
- CNS stimulant
| - appetite suppressant
29
Tx ADHD
amphetamine like drug: METHYLPHENIDATE
30
Function of modafinil
- inhibit NET and DAT-> increase synaptic NE, dopamine, serotonin, and glutamate
- decrease GABA
31
Indirect sympathomimetic drug used for Tx of narcolepsy
MODAFINIL
32
Tyramine present in what foods
```
Cheddar cheese
Maramite
Wine
Country ham
Fava beans
```
33
Patients treated with Mao inhibitors should avoid tyramine containing foods why
(Mao metabolises tyramine)
| Mao inhibitors -> increased effects of tyramine-> hypertension
34
Catecholamine reuptake inhibitors ( Indirect sympathomimetic)
```
TCA -imipramine
Atomoxitine, reboxitine
Sibutramine
Duloxitine
Cocaine
```
35
Is an NE and serotonin reuptake inhibitors cause side effects of orthostatic tachycardia and used to treat urinary incontinence
TCA- imipramine
36
NET inhibitor used to treat ADHD
Atomoxitine
37
Drugs used to treat ADHD
1. Methylphenidate (amphetamine like)
| 2. Atomoxitine (NET inhibitor)
38
Serotonin and NE reuptake inhibitor used to as appetite suppressant in obesity
Sibutramine
39
Function and use of duloxitine
1. NE and serotonin reuptake inhibitor
2. antidepressants
3. Treat fibromyalgia ( musculoskeletal pain)
40
Cocaine effects
```
Sympathomimetic inhibiting reuptake of NE and especially dopamine in the CNS
Effects: - increase vasoconstriction
- hypertension
- angina pectoris
- mucosal rupture
```
41
Central anti-adrenergic
```
They are alpha 2 agonist of CNS:
Clonidine
Guanabenz
Guanfacine
Methyldopa ( alpha methylnorepinephine)
```
42
Function of central anti adrenergic
Dec sympathetic outflow from CNS
cause orthostatic Hypotension
Clonidine- can also cause rebound HPT, sedation
43
Peripheral presynaptic adrenergic
Dec NE->Dec bp, orthostatic Hypotension, increase GI motility, Dec urinary retention, bradycardia
Guanethidine - increase infusion-> Dec NE
Guanadrel- same
Bretylium-same and used as antiarrhythmics
Reserpine- block VMAT
44
Postsynaptic alpha antagonist
```
Phentolamine
Phenoxybenzamine
Prazosin
Doxaosin
Terazosin
Tamsulosin
```
45
Phentolamine function and use
```
Antagonist of alpha 1 and alpha 2
- Dec PVR
- hypotension
- antagonises effect of serotonin
- reflex cardiac stimulation ( angina pectoris, arrhythmia)
Uses:. 1.Tx pheochromocytoma
2. Tx cocaine toxicity
3. Tyramine toxicity in patients tx w/ MAO inhibitor
```
46
Side effects of chronic use of phentolamine
Abdominal cramping
Ulceration
Diarrhea
47
Phenoxybenzamine action and function
Is no reversible Acts on both alpha 1and 2 receptors present on postsynaptic and presynaptic terminal
- cause dec in vasoconstriction
- orthostatic Hypotension
- tx for pheochromocytoma
48
Prazosin action, uses, side effects
Antagonist Acts on alpha 1 receptors
- orthostatic Hypotension
- reflex tachycardia
Use:1. tx for PTSD
2. Tx hypertension
3. Tx CHF
effects: 1.can cause Prazosin Syncope
2. Chronic use reduce efficacy
49
Terazosin and doxazosin use
Alpha 1 Antagonist used to tx BPH
50
Tamsulosin features and use
Alpha 1 Antagonist with high BA and t1/2 9-15hrs
Inhibit contraction of prostate-> tx BPH
51
Alpha 2 antagonist
Yohimbine
| Mert something check sketchy
52
Action of yohimbine and use
Alpha 2 antagonist, blocks alpha 2 receptors in medulla in CNS and presynaptic terminal in the periphery -> increase NE release
1. Increases BP
2. aphrodisiac- tx ED
53
Quinazoline derivative and use
Prazosin (piperazinyl quinazoline)
Silodosin
Alfuzosin
Indoramin
Tx: BPH
And increase risk of prolonged QT
54
Labetalol
Alpha 1 and beta antagonist
55
Chlorpromazine and haloparidol
Act at dopamine receptor and alpha receptor antagonist
56
Ergot derivatives: ergotamine and dehydroegrotamine
Reversible alpha receptor blockage-> partial agonist effect
57
Pharmacokinetics of beta antagonist drugs
1. Increase absorption by oral route
2. Low BA
3. Rapid distribution-> large Vd
58
Actionof beta blockers
1. Dec heart rate and contractility and BP
2. Increase resp tone
3. Anti arrhythmic
4. Tx angina pectoris (Dec heart O2 demand), cardiac obstructive hypertrophy,
5. Tx thyrotoxicosis, anxiety, migraine
6. Local anesthetic
7. Antihypertensive (Dec renin)
8. Aortic dissection
9. Long term use-> Dec mortality in MI, myocardial arrhythmias
10. Dec lipolysis, gluconeogenesis-> hypoglycemia ( tx with glucagon)
59
Side effect of beta blocker
1. Worsen heart failure
2. Dec AV conduction
3. Respiratory obstruction in patients w/lung disease
4. Vivid dreams, nightmares, fatigue, and cold extremities
60
Metaprolol
Beta 1 selective antagonist
- tx acute MI, cardiac congestion
- less effect on asthmatic patients
61
Atenolol
Beta 1 selective antagonist
- do not pass BBB
- manage hypertension
62
Timolol
Non selective beta blocker
- tx glaucoma ( Dec production of aqueous humor)
- topical effect
63
Pindolol
Beta antagonist and partial agonist
64
Nevibolol
Highly selective beta 1
| - increase vasodilation -> effect endothelium to produce increase NO
65
Nadolol
Non selective beta blocker
Longer duration of action
Tx glaucoma
66
Mixed alpha1 and beta antagonist
Labetalol
| Carvedolol
67
Dopamine receptor action and gprotein
D1 is Gs- vasodilation
| D2 is Gi- emesis, inhibition of prolactin
68
Dopamine agonist
Fenoldopam- tx hypertension, heart failure, and MI, diuretic.
69
Tx for Parkinson's disease
D2 agonist:
Levadopa
Apmorphine
Bromocriptine
70
Metoclorprimidine and domperidone
D2 antagonist
- increase peristalsis
- increase gastric emptying
- constrict sphincter -tx GERD
- block D2 receptor in CTZ of medulla- antinuasea and antiemetic action
71
Tx orthostatic hypotension
1. Milodrine (alpha 1 agonist)
| 2. Yohimbine (alpha 2 antagonist)
