PHARMACOLOGY- Autonomic drugs Flashcards
(177 cards)
1
Q
Which neurotrasmitter manage parasympathetic effect?
A
ACh
2
Q
Where does parasympathetic has effects?
A
Cardiac and smooth muscle, gland cells, nerve terminalis
3
Q
This is the way of parasympathetic Transmission impulse
A
Medula (first neuron)- Second Neuron (free, Nicotinic receptors)- Organ (Stimulated by ACh, Muscarinic receptors)
4
Q
Who controls the sweat glands?
A
Sympathetic
5
Q
Which is the way of Sweat gland sympathetic stimulation?
A
Medulla (first neuron-ACh) - Ganglia (Second neuron, Nicotinic receptors)- Organ (Stimulated by ACh, Muscarinic receptors)
6
Q
Which Structures are stimulated by Sympathetic in α β receptors?
A
Cardiac and smooth muscle, gland cells, nerve terminals
7
Q
This is the way of sympathetic Transmission impulse until reaching α β receptors
A
Medulla (first neuron-ACh) - Ganglia (Second neuron, Nicotinic receptors)- Organ (Stimulated by NE, α β receptors)
8
Q
Which Structures are stimulated by Sympathetic in D1 receptors?
A
Renal vasculature, smooth muscle
9
Q
This is the way of sympathetic Transmission impulse until reaching D1 receptors
A
Medulla (first neuron-ACh) - Ganglia (Second neuron, Nicotinic receptors)- Organ (Stimulated by Dopamine, α β receptors)
10
Q
Who stimulates adenal medulla?
A
ACh
11
Q
Once stimulated by ACh produced in the Medulla, what does Adrenal Medulla produces?
A
Epinephrine
Norepinephrine
12
Q
Who stimulates the somatic impulse?
A
Voluntary motor nerve
13
Q
Who is the target of Somatic impulse?
A
Skeletal muscle
14
Q
This is the way of Somatic Transmission impulse until reaching Skeletal muscle
A
Medulla (first neuron) ACh and Skleletal muscle (Nicotinic receptors)
15
Q
What is the difference of Sweat glands invervation and Adrenal medulla from other Sympathetic nervous system?
A
Sweat glands and Adrenal medulla are part of the sympathetic nervous system but are innervated by cholinergic fibers
16
Q
What prevents release of neurotransmitter at all cholinergic terminals?
A
Botulinum toxin
17
Q
These are consider cholinergic fibers
A
Parasympathetic
Sweat glands (sympathetic)
Adrenal medula (sympathetic)
Somatic
18
Q
This is the way of Nervous system impulse reachs Adrenal Medulla
A
Medulla (first neuron-ACh) - Adrenal Medulla (Nicotinic receptors)- Secretion of Epi, Ne
19
Q
Which are the receptors of ACh?
A
Nicotinic ACh receptors
Muscarinic ACh receptors
20
Q
These are the subtypes of Nicotinic ACh receptors
A
Nn (found in autonomic ganglia)
Nm (found in neuromuscular junction)
21
Q
Which kind of channels do Nicotinic ACh receptors have?
A
Are ligand gated Na+/ K+ channels
22
Q
Which kind of channels do Muscarinic ACh receptors have?
A
G protein coupled receptors that ussually act through 2nd messengers
23
Q
Which are the subtypes of Muscarinic receptors?
A
M1, M2, M3, M4, M5
24
Q
Who have Muscarinic receptors?
A
Parasympathetic Sweat glands (Sympathetic)
25
Where do Nicotinic receptors are found?
Somatic (Skeletak muscle)
26
These are sympathetic receptors
α1, α2, β1, β2
27
Sympathetic receptor α1, Which kind of G protein class is?
q
28
These are the major functions of Sympathetic receptor α1
↑ vascular smooth muscle concentration,
↑ pupillary muscle contraction (mydriasis)
↑ intestinal and bladder sphincter muscle contraction
29
Which kind of G protein class are Sympathetic receptor α2?
i
30
This is the effect of Sympathetic receptor α2 stimulation
↓ sympathetic outflow
↓ insulin release
↓ lipolysis
↑ platelel aggregation
31
Which kind of G protein class are Sympathetic receptor β1 and β2?
s
32
Which are the effects of β1 receptors stimulation?
↑ heart rate
↑ Contractility
↑ renin release
↑ lipolysis
33
These are the effects of β2 receptors stimulation
```
Vasodilation, bronchodilation
↑ heart rate
↑ Contractility
↑ lipolysis
↑ insulin release
↓ uterine tone (tocolysis)
Ciliary muscle relaxation
↑ aqueous humor production
```
34
Name the parasympathetic receptors
M1, M2, M3
35
What kind of G protein class does each Muscarinic receptor has?
```
M1= q
M2= i
M3= q
```
36
Where are M1 receptors found?
CNS, enteric nervous system
37
This is the effect of M2 receptors stimulation by parasympathetic
↓ Heart rate and contractility of atria
38
Which is the effect of M3 receptors?
↑ exocrine gland secretions (eg lacrimal, salivary, gastric acid)
↑ gut peristalsis
↑ Bladder contraction
bronchoconstriction
↑ pupillary sphincter muscle contraction (miosis)
Ciliary muscle contraction (accomodation)
39
Which is the effect of Dopamine in D1 receptors?
Relaxes renal vascular smooth muscle
40
This is the effetc of Dopamine in D2 receptors
Modulates Transmitter release, especially in brain
41
Which kind of G protein class are Dopamine receptors?
```
D1= s
D2= i
```
42
Name the Histamine receptors
H1
| H2
43
These are histamine receptor G protein class
```
H1= q
H2= s
```
44
Vasopresin receptors
V1
| V2
45
This is the effect of V1 receptor stimulation
↑ vascular smooth muscle contraction
46
What is the effect of V2 receptor stimulation?
↑ H2O permeability and reabsorption in the collecting tubules of the kidney
47
Which receptors are Gq?
H1, α1, V1, M1, M3
48
This is the process of how receptor that have G protein class produce Smooth muscle relaxation
Receptor → Phospholipase C→ Acts in PIP2 → IP3 → ↑ Ca2+ in → Smooth Muscle relaxation
49
This is the menominc for Gq receptors
HAVe 1 M&M
| H1, α1, V1, M1, M3
50
Which are the two pathways for PIP2?
DAG→ Protein kinase C
| IP3 → ↑ Ca2+ in → Smooth Muscle relaxation
51
These are the receptors associated to Gs
β1, β2, D1, H2, V2
52
Who are the receptors associated to Gi?
M2, α2, D2
53
What is the process after Gs and Gi are stimulated?
Adenylyl cyclase → ATP → cAMP → Proteinkinase A
| Which leads to ↑ Ca2+ in (heart) and Myosin light chain kinase (smooth muscle)
54
How is the process of cholinergic impulse?
Choline is incorporated to the axon → Choline+ Acetyl-CoA→ ACh→ACh incorporated to vesicles→ Liberation of ACh vesicles→ ACh reach the receptor in Post synaptic membrane
55
Who inhibits Choline incorporation to DNA?
Hemicholinium
56
Who can inhibite ACh incorporation to Vesicles?
Vesamicol
57
This cofactor positivively interacts in ACh vesicles liberation
Ca2+
58
Who inhibits ACh liberation in pre synaptic membrane?
Botulinun
59
Which is the process of Noradrenergic impulse until reachinng the receptor?
Tyrosine incorporated to Axon→ Tyrosine → DOPA → Dopamine → NE in vesicles→ liberation of NE in presynaptic membrane→ Adrenoreceptors α or β in post synaptic membrane
60
These are the other outcomes of Noradrenergic secretion
Negative feedback
| Diffusion, metabolism
61
Who modulates release of norepinephrine from a sympathetic nerve ending?
Norepinephrine itself
62
Where does Norepinephrine acts?
On presynaptic α2 autoreceptors, angitensin II and other substances
63
How are cholinomimetic agents classified?
Direct agonist
| Indirect agonists
64
Which drugs are Cholinomimetic Direct agonist?
Bethanechol
Carbachol
Pilocarpine
Methacholine
65
Which is the clinical application for Bethanechol?
Postoperative ileus, neurogenic ileus, and urinary retention
66
Which is the mechanism of Action of Bethanecol?
Activates bowel and bladder smooth muscle; resistant to AChE
67
When is recommended the clinical use for Carbachol?
Glaucoma, pupillary constriction, and relief of intraocular pressure
68
This is the clinical application for Pilocarpine
Potent stimulator of sweat, tears and saliva
| Open angle and closed angle glaucoma
69
This is the mechanism of action of pilocarpine
Contracts ciliary muscle of eye (open angle glaucoma), pupillary sphincter (closed angle glaucoma)
70
Direct Agonist used as Challenge test for diagnosis of astha
Methacholine
71
What is the action of Methacoline?
Stimulates muscarinic receptors in airway when inhaled
72
Alternative name for Indirect agonist
Anticholinesterases
73
Name anticholinesterase drugs
```
Neostigmine
Pyridostigmine
Physostigmine
Donepezil
Rivastigmine
Galantamine
Edrophonium
```
74
These are the clinical use for Neostigmine
Postoperative and neurogenic ileus and urinary retention
Myasthenia gravis
Reversal of neuromuscular junction blockade (postoperative)
75
Which is the effect of Neostigmine?
↑ Endogenous ACh
76
How much penetreation does Neostigmine has to CNS?
No CNS penetration
77
When is recommended to use Pyridostigmine?
```
Myastenia gravis (long acting)
Does not penetrate CNS
```
78
This is the effect of Pyridostigmine
↑ Endogenous ACh
79
Which is the effect of all Cholinomimetic indirect antagonists?
↑ Endogenous ACh
80
What is different in Physostigmine compared to other Anticholinesterases drugs?
Anticholinergic toxicity (crosses blood brain barrier → CNS)
81
Which clinical use does Physostigmine has?
For atropine overdose
82
Which anticholinesterase drugs are used for Alzheimer disease?
Donepezil
Rivastigmine
Galantamine
83
Historically, diagnosis of myasthenia gravis (extremely short acting)
Edrophonium
84
How is Myastenia gravis nowdays diagnose?
By antiAChR Ab (anti-acetylcholine receptor antibody) test
85
Before administering Cholinomimetic agents we need to be careful for...
Watch exacerbation of COPD, asthma, and peptic ulcers when giving to susceptible patients
86
When is often to see Cholinesterase inhibitor poisoning?
Often due to organophosphates, such as parathion, that irreversibly inhibit AChE
87
These are the clinical manifestations of Cholinesterase inhibitor poisoning
```
DUMBBELSS
Diarrhea
Urination
Miosis
Bronchospasm
Bradycardia
Excitation of skeletal muscle and CNS
Lacrimation
Sweating
Salivation
```
88
Where can we find organophosphates?
Insecticides
89
Who usually suffer organophospate poisoning?
Farmers
90
This is the antidote for Cholinesterase inhibitor poisoning
Atropine (competitive inhibitor)+ pralidoxime (regenerates AChE, if given early)
91
Drugs Consider Muscarinic antagonists
```
Atropine, homatropine, tropicamide
Benztropine
Scopolamine
Ipratropium, tiotropium
Oxybutynin, darifenacin and solfenacin
Glycopyrrolate
```
92
Clinical application for Atropine
To treat Bradycardia
| Produce mydriases and cyclopegia
93
This is the clinical use for Benztropine
Parkinson disease
94
Muscarinic antagonist for motion sickness
Scopolamine
95
Which family are Ipratroium, tiotropium?
Muscarinic antagonist
96
Clinical use for Ipratrpium, tiotropium
COPD, asthma
97
These muscarinic antagonists reduce the urgency in mild cystitis and reduce bladder spasms
Oxybutynin, Darifenacin and Solifenacin
| Other agents are Tolterodine, fesoterodine, trospium
98
How can Glycopyrrolate be administered?
Parenteral
| Oral
99
Which is the benefit of using Glycopyrrolate parenteral?
Preoperative use to reduce airway secretions
100
Clinical use of Glycopyrrolate oraly
Drooling, peptic ulcer
101
Which group of drugs is Atropine?
Muscarinic antagonist
102
These are effects in systems with the use of Atropine
```
↑ pupil dilation, cycloplegia
↓ secretions of airway
↓ Acid secretion of Stomach
↓ Gut motility
↓ Urgency in cystitis
```
103
Which receptors mediate Atropine in Skeletal muscle and CNS?
Nicotinic receptors
104
Which are possible toxic effects of Atropine?
↑ body temperature (due to ↓ sweating); rapid pulse; dry mouth; dry, flushed skin; cyclopegia; constipation; disorientation
105
What can Atropine cause in eldery?
Acute angle closure glaucoma (due to mydriasis)
106
In which patients can atropine cause Urinary retention?
Men with prostatic hyperplasia
107
This is a possible side effect of Atropine in infants
Hypertermia
108
What is Jimson weed (Datura)?
Gardeners pupil (mydriasis due to plant alkaloids)
109
Classification of Sympathomimetics
Direct Sympathomimetics
| Indirect Sympathomimetics
110
Name Direct Sympathomimetics drugs
```
Epinephrine
Norepinephrine
Isoproterenol
Dopamine
Dobutamine
Phenylephrine
Albuterol, Salmeterol, Terbutaline
```
111
Which effect does Epinephrine has?
β > α
112
These are applications for Epinephrine
Anaphylaxis
Opne angle glaucome
Asthma
Hypotension
113
When does α effect predominates in epinephrine?
At high doses
114
These are the receptors where norepinephrine acts
α1 > α2 > β1
115
Application for Norepinephrine
Hypotension (but ↓ renal perfussion)
116
In these receptors Isoproterenol has its effects
β1 = β2
117
In this situation Isoproterenol is used
Electrophysiologic evaluation of tachyarrytmhias. Can worsen ischemia
118
These are the receptors for Dopamine
D1= D2 > β > α
119
When is recommended the clinical use of Dopamine?
Unstable bradycaria, heart failurem shock
120
Which effects predominate at high doses of Dopamine?
Inotropic and chronotropic α effects predominate at high doses
121
These are the receptors of Dobutamine
β1 > β2, α
122
Clinical uses for Dobutamine
```
Heart failure (inotropic > chronotropic)
Cardiac stress testing
```
123
Which are the Phenylephrine receptors?
α1 > α2
124
These are the results if Phenylephrine use
Hypotension (Vasoconstrictor), Ocular procedures (mydriatic), rhinitis (decongestant)
125
Direct sympathomimetics that work at β2 > β1
Albuterol, Salmeterol, Terbutaline
126
When is indicated Albuterol?
For Acute asthma
127
Clinical use for Salmeterol
Long term asthma or COPD control
128
When is recommended Terbutaline?
To reduce premature uterine contraction
129
Indirect sympathomimetics
Amphetamine
Ephedrine
Cocaine
130
Effect of Amphetamines
Indirect general agonist, reuptake inhibitor, also releases stored catecholamines
131
Clinical use for Amphetamines
Narcolepsy, Obesity, Attention defficit disorder
132
Which is the effect of Ephedrine?
Indirect general agonist, release stored catecholamines
133
This is the clinical use for Ephedrine
Nasal decongestion, urinary incontinence, hypotension
134
What is Cocaine effect?
Indirect general agonist, reuptake inhibitor
135
Clinical use for Cocaine?
Causes vasoconstriction and local anesthesia
136
If cocaine intoxication is suspected what is contraindicated?
Never give β blockers if cocaine intoxication is suspected
137
What hapens if you give β blockers and the patient has Cocaine intoxication?
Can lead to unopposed α1 activation and extreme hypertension
138
How does Norepinephrine causes bradycardia at the end?
Norepinephrine causes ↑ in systolic and diastolic pressures as a result of α1 mediated vasocontriction → ↑ mean arterial pressure → Bradycardia
139
Which is the mediaction that has oposite effects as Norepinephrine, no longer commonly used?
Isoproterenol
140
How does Isoproterenol produces Increased Heart rate?
Has a little α effect but causes β2 mediated vasodilation, resulting in ↓ mean arterial pressure and ↑ heart rate through β1 and reflexes activity
141
Which receptors are Sympatholytics?
α2 agonists
142
These drugs are Sympatholytics
Clonidine
| α methyldopa
143
Which are the applications of Clonidine?
```
Hypertensive urgency (limited situations); does not decreases renal blood flow
ADHD, severe pain and a variety of offlabel indications (eg ethanol and opiod withdrawal)
```
144
These cases are consider with Clonidine toxicity
CNS depression, bradycardia, hypotension, respiratory depression, and a smell pupil size
145
Sympatholytics used in Hypertension in pregnancy because is safe
α methyldopa
146
When is consider that α methyldopa causes toxicity?
Direct coombs positive, hemolytic anemia. SLE like syndrome
147
This is the classification of α blockers
Non selective
α1 selective
α2 selective
148
α Blockers nonselective
Phenoxybenzamine (irreversible)
| Phentolamine (reversible)
149
When is recommended Phenoxybenzamine? Why?
Pheochromocytoma (used preoperatively) to prevent catecholamine (hypertensive) crisis
150
These are Phenoxybenzamine toxicity manifestations
Orthistatic hypotension, Reflex tachycardia
151
In this situations you can administer Phentolamine
On MAO inhibitors who eat tyramine- containing foods
152
Which drugs are α1 selective?
Prazosin
Terazosin
Doxazosin
Tamsulosin
153
Clinical use for α1 selective blockers
Urinary symptos of BPH
| Hypertension
154
This is the only α1 selective blockers that is not recommended for hypertension
Tamsulosin
155
In this case Prazosin is recommended
PTSD (Post-traumatic stress disorder)
156
α2 selective blocker used for depression
Mirtazapine
157
Side effects of Mirtazapine
Sedation, ↑ Serum cholesterol, ↑ Apetite
158
Name β blockers
Metoprolol, Acebutol, btaxolol, carvedilol, esmolol, nadolol, timolol, pindolol, labetalol
159
Applications of β blockers
```
Angina Pectoris
MI
SVT
Hypertension
CHF
Glaucoma
```
160
How do β blockers act in Angina pectoris?
↓ Heart rate and contractility, resulting in ↓ O2 consumption
161
Which β blockers are used for MI?
Metoprolol
Carvedilol
Bisoprolol
Decrease mortality
162
Which β blockers are used for SVT?
Metoprolol
| Esmolol
163
How are β blockers classified for SVT (Supraventricular Tachycardia) treatment
Class II antiarrhythmic
164
Which is the mechanism of antiarrythimc for β blockers?
↓ AV conduction velocity
165
How do β blockers work in Hypertension?
↓ Cardiac output, ↓ renin secretion
166
Which receptors are blockade by β blockers in order to decrease Renin secretion?
β1 receptor blockade on JGA cells
167
What is the purpose to give β blockers in CHF?
Slows progression of chronic failure
168
Which β blocker is recommended for Glaucoma?
Timolol
169
This is the effect of Timolol in the treatment of Glaucoma
↓ Secretion of aqueous humor
170
These are possible secondary effects of β blockers
Incompetence
Cardiovascular adverse effects (bradycardia, AV block, CHF)
CNS adverse effects (seizures, sedation, sleep alterations)
Asthmatics/ COPDers (may cause exacerbation)
171
Which β blocker can cause Dyslipidemia?
Metoprolol
172
When is recommended to avoid β blockers?
Avoid cocaine users due to risk of unopposed α adrenergic receptor agonist activity
173
Which is the relationship of β blockers and Diabetes?
Despite theoretical concern of masking hypoglecemia in diabetics, benefits likely outweigh risks; not contraindicated
174
Which drugs are β1 selective antagonist (β1>β2)?
```
Acetabutolol (partial agonist)
Atenolol
Betaxolol
Esmolol
Metoprolol
```
175
β blockers Nonselective antagonist (β1= β2)
Nadolol
Pindolol (partial agonist)
Propanolol
Timolol
176
Nonselective α and β antagonist
Carvedilol
| Labetalol
177
Which is the effect of Nebivolol?
Combines Cardiac β1 adrenergic blockade with stimulation of β3 receptors, which activate nitric oxide synthase in the vasculature
