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pharmacology final ( 1st sem) > B: 1-7 > Flashcards

B: 1-7 Flashcards

1
Q

M1-R location

A

Nerve endings

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2
Q

M2-R location

A

Heart
some nerve endings

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

Arterial 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
Q

Near vision

A

↑ M3 tone will contract ciliary muscle
Spherical lens

ciliary m contraction > decrease the diameter of the ring of ciliary muscle causing relaxation of the zonule fibers
the lens becomes more spherical, increasing its power to refract light for near visio

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26
Q

Miosis

A

M3 ↑

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27
Q

How to lower aqueous humor production?

A

a2 agonist

B2 antagonist

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28
Q

Cholinomimetics

A
  • Choline esters: Acetylcholine, Bethanechol, Carbachol, metacholine
  • Alkaloids: Muscarine, Nicotine, pilocarpine
  • Synthetic: Vareniciline
  • Carbamates: Neo, Pyrido, Riva -stigmine
  • Organophosphates: Malathion, Sarin
  • Alcohol: Edrophonium, donepezil
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29
Q

Carbachol receptor preferance

A

M=N

קר בחול אז בוא נשחק יפה ביחד

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30
Q

Bethanechol receptor preferance

A

M

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31
Q

Pilocarpine receptor preferance

A

M

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32
Q

Carbachol indications

A

Glaucoma

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33
Q

Which direct acting cholinomimetic is resistance to acetylcolinesterase?

A

Carbachol

כל כך קר אז אף אחד לא מתקרב אליו

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34
Q

Carbachol

How to give

A

Topical

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35
Q

Pilocarpine drug properties

A

Oral, I.M , topical in eye
Lipd soluble
30min-2h duration of action

activates muscarinic receptor ( increa IP3 + DAG)
may also activate EPSP s via M-R in ganglia

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36
Q

dry mouth is also called

A

Xerostomia

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37
Q

Pilocarpine indications

A

Glaucoma
Xerostomia
Incuced sweat test in CF

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38
Q

What is the difference btw. tertiary and quaternary amine?

A

Tertiary freely cross the BBB

זה יותר קטן אז הוא מצליח לעבור

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39
Q

Which Carbamates are tertiary amine?

A

Physostigmine

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40
Q

Physostigmine indications

A

Antidote in case of Atropine overdose

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41
Q

Neostigmine duration of action and indication

A

2-4 h

MG (treatment)
Non obstructive ileus
Urinary retention
Reversal of N(M) block –> in surgery anesthesia

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42
Q

Pyridostigmine duration of action and indication

A

4-8 h

MG

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43
Q

Which has a longer duration of action?

Pyridostigmine
Neostigmine

A

Pyridostigmine

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44
Q

Rivastigmine properties as a drug

A

Lipid soluble
Cross CNS
Given as transdermal patch

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45
Q

Rivastigmine indications

A

Alzheimer’s disease

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46
Q

Edrophonium indications

A 
Diagnosis of MG
Tensilon test (MB Vs. Cholinergic crisis)

cholinergic crisis gets worse

MG= antibodies against postsynaptic acetylcholine receptor.

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47
Q

AchE inhibitiors poisoning

A

DUMBBLES

Diarrhea
Urination
Miosis
Bradycardia
Bronchoconstriction
Excitation
Lacrimation
Secretion
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48
Q

Excesp for AchE inhibitor, what else will you give to a MG patient?

A

Selective muscarinic antagonist to control muscarinic side effects like GI

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49
Q

Non selective muscarinic antagonists

A 
Atropine
Butyl-scopolamine
Scopolamine
Cyclopentolate
Procyclidine
50
Q

Modest selectivity to M3 muscarinic antagonist

A

Solifenacin

51
Q

What is the difference btw. Ipratropium to Tiotropium?

A

Ipratropium: Non selective. Shorter action
Tiotropium: M3 selective. Longer action

52
Q

Duration of action of Atropine?

A

2-4 h

Mydriasis effect for even 8 days ( >72hr)

53
Q

Atropine indications

A
  • Opthalmology (mydriasis, cycloplegia) >72 hr
  • Antidote for ChE inhibitors toxicity

Anti-diarrheal
Anti-spasmodic
Anti-secretery
Bradyarrhythmias

54
Q

Cyclopentolate indications

A

topical Opthalmology to produce mydriasis and cycloplegia

Cyclo-round like the eyes

55
Q

Scopolamine molecule features

Indications

A

Lipid soluble, can enter the CNS

Motion sickness
Transdermal patch

Suck it up! its only water

56
Q

Butyl-scopolamine molecule features

Indications

A

No CNS entry

Pain from GI/GU spasmodic activity (Like menstrual cramps)

Buty female period

57
Q

Procyclidine
administration
molecule features
Indications

A

Lipid soluble, enter CNS
Oral, perenteral

Parkinson disease
Extrapyramidal disorders

58
Q

Whcih Muscarinic antagonists can treat Parkinson

A

Procyclidine

59
Q

Solifenacin
Oxybutynin

molecule features
Indications

A

Oral, ransdermal patch

Bladder spasms
Urinary incontinence

כי הם ספציפיים לאמ3

Solifenacin (m3 selective)
Oxybutynin (non selective antimuscarinic)

60
Q

Ipratropium
Tiotropium

Indications

A

Bronchodilator for asthma/COPD

61
Q

Which is M3 selective?

Ipratropium
Tiotropium

A

Tiotropium

62
Q

Adverse effects of Muscarinic antagonists?

A 
↓ Secretion
Mydriasis, cyclpolegia
Glaucoma exxacerbation
Tachycardia
CNS effects
Urinary retention
Constipation
63
Q

Chemical antagonist for organophosphate

A

Pralidoxime

64
Q

Epinephrine is produced by

A

Exclusively by the medulla of the adrenal gland

65
Q

NE is produced by

A

Medulla of the adrenal gland

Sympathetic NS

66
Q

Epinephrine low dose

A

B1, B2 stimulation mainly:
HR, SV, CO, pulse pressure ↑
TPR, BP ↓
Bronchodilation

67
Q

Epinephrine high dose

A

a1 stimulation mainly:
TPR, BP ↑
Reflex bradycardia

68
Q

Epi indications

A 
Cardiac arrest
Heart block
Anaphylactic shock
Hypotensive emergency
Adjucent to local anesthetics (↓ local blood flow)
69
Q

Epi side effects

A 
HTN
Arrhythmias
Stroke
MI
Pulmonary edema
70
Q

NE receptor preferance

A

a1, a2, B1

71
Q

NE indications

A 
Cardiac arrest
Heart block
Hypotensive emergency
Adjucent to local anesthetics (↓ local blood flow)
Shock
72
Q

NE- What type of shock is it used in?

A

Cardiogenic
Neurogenuc
Septic

73
Q

NE side effects

A 
Vasospasms
Tissue necrosis
HTN
Arrhythmias
MI
74
Q

Dopamine dose dependent effect

A

Low dose: D1 → renal perfusion ↑
Medium: B1 stimulation → cardiac ↑
High: Acts like Epi (Loses selectivity)

75
Q

Dopamine indications

A

Shock (with renal failure)

76
Q

Dopamine side effects

A

Arrhythmias

77
Q

Isoprenaline receptor preferance

A

B1 = B2

78
Q

Isoprenaline indications

A

Cardiac arrest
Complete heart block
Acute asthma attack

79
Q

Dobutamine receptror preferance

A

B1 > B2&raquo_space;> a1

80
Q

Dobutamine indications

A

Cardiogenic shock
Acute heart failure
Cardiac stimulation in cardiac stress test

81
Q

a agonists
+
Which a?

A 
Phenylephrine: a1
Oxymetazoline: Local a1, systemic a2
Clonidine: a2, I2
Rilmenidine: a2, I2
Methyldopa: a2

POC RM

82
Q

a2 agonists

A

Oxymetazoline (also a1)
Clonidine
Rilmenidine
Methydopa

83
Q

a1 agonists

A

Phenylephrine

Oxymetazoline- locally

84
Q

Special feature of Phenylephrine

A

Not inactivated by COMT → longer duration of action compared to catecholamines

85
Q

Phenylephrine duration of action

A

15-60 min

86
Q

Phenylephrine indications

A

Opthalmologic (mydriasis)
Decongestant
Hypotension (TPR, mean BP↑)

87
Q

Phenylephrine side effects

A 
Reflex bradycardia
HTN
Stroke
MI
Ischemic necrosis of mucus memb.
88
Q

Oxymetazoline indications

A

Topical decongestant

89
Q

Oxymetazoline side effects

A

When given systemically due to a2 activation (Hypotension)

90
Q

Clonidine receptor preferance

A

a2

I2

91
Q

Clonidine drug features
Molecule?
How to give?

A

Imidazole derivative

Oral, Treansdermal patch

92
Q

Clonidine indications

A

Antyhypertensive
ADHD
Turettes syndrome
Alcohol withdrawal syndrome

93
Q

Clonidine side effects

A

Sedation
Dry mouth
Severe rebound HTN when sudddenly stopped
Drug induced lupus

94
Q

Which are the a2, I2 agonists?

A

Clonidine

Rilmenidine

95
Q

Rilmenidine indications

A

Antihypertensive

96
Q

Rilmenidine side effects

A

Milder compared to Clonidine

97
Q

Pure a1 agonist

A

Phenyephrine

98
Q

Pure a2 agonist

A

Methyldopa

(Brimonidine, : a2-selective agonists appear to
reduce synthesis of aqueous humor

Tizanidine: an imidazoline related to clonidine reinforces presynaptic inhibition in
the spinal cord

99
Q

Methyldopa drug features

A

Prodrug: Transported into the brian and converted to methyl-NE

100
Q

Methyldopa indications

A

Antihypertensive

101
Q

Methyldopa side effects

A

Sedation
Induces hemolytic antibodies

Drug induced lupus

102
Q

Which release inducing agent do you know?

A

Tyramine
Ephedrine
Amphetamine

TEA

103
Q

Ephedrine indications

A
  • narcolepsy,
  • idiopathic postural hypotension,
  • enuresis = involuntary urination
Stimulant
Appetite suppressant
Concentration aid
Decongestant
Hypotension associated woth anaesthesia
Less addictive than Amphetamines
104
Q

Non selective a-R antagonists

A

Phentolamine: Competitive
antagonist at a
receptors

Phenoxybenzamine: Irreversible (covalent}
binding to a receptors

105
Q

How to give Phentolamine?

What is the duration of action?

A

Oral: 20-40 min
Parenterally: 2-4 h

106
Q

What is the difference btw. Phentolamine and Phenoxybenzamine?

A

Phenoxybenzamine binds the a-R irreversibely

107
Q

Phentolamine indications

A

Pre-operative management of Pheochromocytoma

Antidote in case of acute HTN due to a agonist overdose

108
Q

Phentolamine side effects

A

Orthostatic hypotension with subsequent reflex tachycardia

109
Q

a1 selective antagonists

A

Prazosin

Doxazosin

Tamsulosin (approved for only BPH bcz partially selective)

110
Q

Prazosin
Tamsulosin
Doxazosin

How to give? Duration of action?

A

Oral

prazosin : 8hr

Doxazosin., tamsulosin : 12-24 hrs

111
Q

Prazosin
Tamsulosin
Doxazosin

Indications

A

HTN
BPH
Prazosin for PTSD

112
Q

Prazosin
Tamsulosin
Doxazosin

Side effects

A

Orthostatic hypotension

113
Q

Which drug is a1 antagonist and weak a2 agonist?

A

Urapidil

114
Q

Urapidil receptor preferance

A

a1 antagonist
a2 weak agonist
5-HT weak agonist
B antagonist

115
Q

Urapidil indications

A

HTN
Hypertensice crisis
BPH

116
Q

Carvedilol receptor preferance

A

B1, B2, a1 antagonist

117
Q

Which drugs are B1, B2, a1 antagonist

A

Carvedilol

Labetalol

118
Q

Carvedilol
Labetalol

How to give?
Duration of action?

A

Oral, IV

5 h

119
Q

Carvedilol indications

A

Congestive HF

**Reduces mortality!

120
Q

Special feature of Carvedilol?

A

Reduces mortality in Congestive HF patients

pharmacology final ( 1st sem) (15 decks)

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