B: 1-7 Flashcards

1
Q

M1-R location

A

Nerve endings

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2
Q

M2-R location

A

Heart

I love you! M2

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3
Q

M3-R location

A

Effector cells
Smooth muscles
Glands
Endothelial cells

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4
Q

a1-R action

A

Arterail and venous contraction
Mydriasis
Urinary spinchter contraction

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5
Q

a2-R action

A

Central and peripheral presynaptic inhibition
↓ insulin release
↓ lipolysis and FFA release
↓ Aqueous humor production

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6
Q

B1-R action

A

↑ SA, AV rate and automaticity
↑ Cardiac contractility
↑ Renin release

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7
Q

B2-R action

A
Peripheral vasodilation
Bronchodilation
↑ Insulin release
↑ Lipolysis and FFA release
↑ Heptaic gluconeogenesis+ Glycogenolysis
↑ Aqueous humor production
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8
Q

B1 effect on the heart SA, AV rate and automaticity=

A

Positive chronotopic effect

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9
Q

Nicotinic N-R location

A

ANS ganglia

Adrenal medula

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10
Q

Nicotinic M-R location

A

Neuromascular end plate

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11
Q

Which factors contribute to the Cholinergic presynaptic inhibatory effect?

A
a2
M2
Hemicholinium
Vasamicol
Botulinum toxin
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12
Q

Which factors contribute to the Cholinergic presynaptic stimulatory effect?

A
M1
B2
AT1
4-Aminopyridine
Latrotoxin
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13
Q

Hemicholinium blocks

A

Choline/Na+ cotransporter

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14
Q

4-Aminopyridine MOA

A

Inhibitis K+ ch → Depol. → Neutransmittr release

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15
Q

Which factors contribute to the Adrenergic presynaptic inhibatory effect?

A
a2
M2
H3
Metyrosine
Reserpine
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16
Q

Which factors contribute to the Adrenergic presynaptic stimulatory effect?

A
B2
M1
AT1
4-Aminopyridine
Latrotoxin
Indirect acting sympathomimetics
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17
Q

Reserpine MOA

A

Inhibitis VMAT

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18
Q

Metyrosine MOA

A

Inhibitis Tyrosine hydroxylase

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19
Q

Iris radial muscle are controlled by

Dilated pupil is also called

A

a1
Mydriasis

Ayi see you 1

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20
Q

Iris circular muscle are controlled by

Constricted pupil is also called

A

M3

Myosis

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21
Q

Ciliary muscles are innervated by

A

B- relaxation
M3- contraction

איריס היא אמא לשלושה ילדים

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22
Q

Bladder wall is innervated by

A

B2- Relax

M3- Contracts

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23
Q

Penis innervation

A

a- ejaculation

M- erection

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24
Q

Far vision

A

↓ M3 tone will relax ciliary muscle

Flat lens

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25
Near vision
↑ M3 tone will contract ciliary muscle | Spherical lens
26
Miosis
M3 ↑
27
How to lower aqueous humor production?
a2 agonist | B2 antagonist
28
Cholinomimetics
Choline esters: Acetylcholine, Bethanechol, Carbachol Alkaloids: Muscarine, Nicotine, pilocarpine Synthetic: Vareniciline Carbamates: Neo, Pyrido, Riva -stigmine Organophosphates: Malathion, Sarin Alcohol: Edrophonium
29
Carbachol receptor preferance
M=N קר בחול אז בוא נשחק יפה ביחד
30
Bethanechol receptor preferance
M
31
Pilocarpine receptor preferance
M
32
Carbachol indications
Glaucoma
33
Which direct acting cholinomimetic is resistance to acetylcolinesterase?
Carbachol כל כך קר אז אף אחד לא מתקרב אליו
34
Carbachol | How to give
Topical
35
Pilocarpine drug properties
Oral, Parentral Lipd soluble 30 min - 2h duration of action
36
dry mouth is also called
Xerostomia
37
Pilocarpine indications
Glaucoma Xerostomia Incuced sweat test in CF
38
What is the difference btw. tertiary and quaternary amine?
Tertiary freely cross the BBB זה יותר קטן אז הוא מצליח לעבור
39
Which Carbamates are tertiary amine?
Physostigmine
40
Physostigmine indications
Antidote in case of Atropine overdose
41
Neostigmine duration of action and indication
2-4 h MG Non obstructive ileus Urinary retention Reversal of N(M) block
42
Pyridostigmine duration of action and indication
4-8 h MG
43
Which has a longer duration of action? Pyridostigmine Neostigmine
Pyridostigmine
44
Rivastigmine properties as a drug
Lipid soluble Cross CNS Given as transdermal patch
45
Rivastigmine indications
Alzheimer's disease
46
Edrophonium indications
``` Diagnosis of MG Tensilon test (MB Vs. Cholinergic crisis) ```
47
AchE inhibitiors poisoning
DUMBBLES ``` Diarrhea Urination Miosis Bradycardia Bronchoconstriction Excitation Lacrimation Secretion ```
48
Excesp for AchE inhibitor, what else will you give to a MG patient?
Selective muscarinic antagonist to control muscarinic side effects like GI
49
Non selective muscarinic antagonists
``` Atropine Benztropine Butyl-scopolamine Cyclopentolate Scopolamine Procyclidine ```
50
Modest selectivity to M3 muscarinic antagonists
Solifenacin | Oxybutynin
51
What is the difference btw. Ipratropium to Tiotropium?
Ipratropium: Non selective. Shorter action Tiotropium: M3 selective. Longer action
52
Duration of action of Atropine?
2-4 h | Mydriasis effect for even 8 days
53
Atropine indications
``` Opthalmology Antidiarrheal Antispasmodic Antisecretery Bradyarrhythmias Antidote for cholinesterase inhibitors toxicity ```
54
Cyclopentolate indications
Opthalmology Cyclo-round like the eyes
55
Scopolamine molecule features | Indications
Lipid soluble, can enter the CNS Motion sickness Transdermal patch Suck it up! its only water
56
Butyl-scopolamine molecule features | Indications
No CNS entry Pain from GI/GU spasmodic activity (Like menstrual cramps) Buty female period
57
Procyclidine Benztropine molecule features Indications
Lipid soluble, enter CNS Oral, perenteral Parkinson disease Extrapyramidal disorders
58
Whcih Muscarinic antagonists can treat Parkinson
Procyclidine | Benztropine
59
Solifenacin Oxybutynin molecule features Indications
Oral, ransdermal patch Bladder spasms Urinary incontinence כי הם ספציפיים לאמ3
60
Ipratropium Tiotropium Indications
Bronchodilator for asthma/COPD
61
Which is M3 selective? Ipratropium Tiotropium
Tiotropium
62
Adverse effects of Muscarinic antagonists?
``` ↓ Secretion Mydriasis, cyclpolegia Glaucoma exxacerbation Tachycardia CNS effects Urinary retention Constipation ```
63
Chemical antagonist for organophosphate
Pralidoxime
64
Epinephrine is produced by
Exclusively by the medulla of the adrenal gland
65
NE is produced by
Medulla of the adrenal gland | Sympathetic NS
66
Epinephrine low dose
B1, B2 stimulation mainly: HR, SV, CO, pulse pressure ↑ TPR, BP ↓ Bronchodilation
67
Epinephrine high dose
a1 stimulation mainly: TPR, BP ↑ Reflex bradycardia
68
Epi indications
``` Cardiac arrest Heart block Anaphylactic shock Hypotensive emergency Adjucent to local anesthetics (↓ local blood flow) ```
69
Epi side effects
``` HTN Arrhythmias Stroke MI Pulmonary edema ```
70
NE receptor preferance
a1, B1, a2
71
NE indications
``` Cardiac arrest Heart block Hypotensive emergency Adjucent to local anesthetics (↓ local blood flow) Shock ```
72
NE- What type of shock is it used in?
Cardiogenic Neurogenuc Septic
73
NE side effects
``` Vasospasms Tissue necrosis HTN Arrhythmias MI ```
74
Dopamine dose dependent effect
Low dose: D1 → renal perfusion ↑ Medium: B1 stimulation → cardiac ↑ High: Acts like Epi (Loses selectivity)
75
Dopamine indications
Shock (with renal failure)
76
Dopamine side effects
Arrhythmias
77
Isoprenaline receptor preferance
B1 = B2
78
Isoprenaline indications
Cardiac arrest Complete heart block Acute asthma attack
79
Dobutamine receptror preferance
B1 > B2 >>> a1
80
Dobutamine indications
Cardiogenic shock Acute heart failure Cardiac stimulation in cardiac stress test
81
a agonists + Which a?
``` Phenylephrine: a1 Oxymetazoline: Local a1, systemic a2 Clonidine: a2, I2 Rilmenidine: a2, I2 Methyldopa: a2 ``` POC RM
82
a2 agonists
Oxymetazoline (also a1) Clonidine Rilmenidine Methydopa
83
a1 agonists
Phenylephrine | Oxymetazoline- locally
84
Special feature of Phenylephrine
Not inactivated by COMT → longer duration of action compared to catecholamines
85
Phenylephrine duration of action
15-60 min
86
Phenylephrine indications
Opthalmologic (mydriasis) Decongestant Hypotension (TPR, mean BP↑)
87
Phenylephrine side effects
``` Reflex bradycardia HTN Stroke MI Ischemic necrosis of mucus memb. ```
88
Oxymetazoline indications
Topical decongestant
89
Oxymetazoline side effects
When given systemically due to a2 activation (Hypotension)
90
Clonidine receptor preferance
a2 | I2
91
Clonidine drug features Molecule? How to give?
Imidazole derivative | Oral, Treansdermal patch
92
Clonidine indications
Antyhypertensive ADHD Turettes syndrome Alcohol withdrawal syndrome
93
Clonidine side effects
Sedation Dry mouth Severe rebound HTN when sudddenly stopped Drug induced lupus
94
Which are the a2, I2 agonists?
Clonidine | Rilmenidine
95
Rilmenidine indications
Antihypertensive
96
Rilmenidine side effects
Milder compared to Clonidine
97
Pure a1 agonist
Phenyephrine
98
Pure a2 agonist
Methyldopa | Brimonidine, Tizanidine
99
Methyldopa drug features
Prodrug: Transported into the brian and converted to methyl-NE
100
Methyldopa indications
Antihypertensive
101
Methyldopa side effects
Sedation | Drug induced lupus
102
Which release inducing agent do you know?
Ephedrine Amphetamine Tyramine
103
Ephedrine indications
``` Stimulant Appetite suppressant Concentration aid Decongestant Hypotension associated woth anaesthesia Less addictive than Amphetamines ```
104
Non selective a-R antagonists
Phentolamine | Phenoxybenzamine
105
How to give Phentolamine? | What is the duration of action?
Oral: 20-40 min Parenterally: 2-4 h
106
What is the difference btw. Phentolamine and Phenoxybenzamine?
Phenoxybenzamine binds the a-R irreversibely
107
Phentolamine indications
Pre-operative management of Pheochromocytoma | Antidote in case of acute HTN due to a agonist overdose
108
Phentolamine side effects
Orthostatic hypotension with subsequent reflex tachycardia
109
a1 selective antagonists
Prazosin Tamsulosin Doxazosin
110
Prazosin Tamsulosin Doxazosin How to give? Duration of action?
Oral 8-24 h
111
Prazosin Tamsulosin Doxazosin Indications
HTN BPH Prazosin for PTSD
112
Prazosin Tamsulosin Doxazosin Side effects
Orthostatic hypotension
113
Which drug is a1 antagonist and weak a2 agonist?
Urapidil
114
Urapidil receptor preferance
a1 antagonist a2 weak agonist 5-HT weak agonist B antagonist
115
Urapidil indications
HTN Hypertensice crisis BPH
116
Carvedilol receptor preferance
B1, B2, a1 antagonist
117
Which drugs are B1, B2, a1 antagonist
Carvedilol | Labetalol
118
Carvedilol Labetalol How to give? Duration of action?
Oral, IV | 5 h
119
Carvedilol indications
Congestive HF | **Reduces mortality!
120
Special feature of Carvedilol?
Reduces mortality in Congestive HF patients