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Pharmacology MBBS > ANS-2 > Flashcards

ANS-2 Flashcards

1
Q

Vasomotor reversal (VMR) of Dale

A

BP variation in a living system when epinephrine + α blocker is given
No rise in BP initially
Delayed decrease due to β2

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2
Q

Dopamine and dose dependent property

A

Dopamine is selective towards certain receptors in certain concentrations

0-2 mcg/kg/min ➡️ D1
2-10 mcg/kg/min ➡️ β1
>10 mcg/kg/min ➡️ α1

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3
Q

Major effects of dopamine at various concentrations

A

0-2 mcg/kg/min ➡️ D1 ➡️ diuresis ➡️ oliguria

2-10 mcg/kg/min ➡️ β1 ➡️ increased cardiac contraction ➡️ CHF

> 10 mcg/kg/min ➡️ α1 ➡️ vasoconstriction ➡️ cardiogenic shock

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4
Q

Dopamine is DoC in

A
  1. Oliguria with CHF

2. Cardiogenic shock (over norepinephrine)

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5
Q

Route of administration of dopamine

Side effect of dopamine

A

Continuous IV infusion (like dobutamine) since it has a very low half life

Arrhythmia (β1 stimulation)

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6
Q

Dobutamine

Uses

A

Exogenous catecholamine
Agonist of β1&raquo_space;> β2
No net effect at α1 (the 2 isomers of the racemic mixture cancel each other)
Uses:
1. Inotrope of choice in acute CHF (without oliguria)
2. Stress echocardiography

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7
Q

Fenoldopam

A
  1. α2 agonist➡️ decreases NE➡️ decreases bp
  2. D1 agonist (like dopexamine)➡️ diuresis➡️ decreases bp

So used in hypertensive emergency (like dopexamine) via IV route

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8
Q

Dopexamine

A
  1. β2 agonist➡️ decreases bp
  2. D1 agonist (like fenoldopam)➡️ diuresis ➡️ decreases bp
    So used in hypertensive emergency (like fenoldopam)
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9
Q

Isoprenaline or isoproterenol

A

Agonist of β1 and β2 receptors
Uses:
1. β1 ➡️ treating bradycardia and AV nodal block
2. β2 ➡️ bronchial asthma

SBP remains normal or increases slightly
DBP decreases
Significant increase in HR (action + feedback regulation due to vasodilation)

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10
Q

Droxedopa

A

Prodrug of NE

Treatment of neurogenic postural hypotension

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11
Q

Drugs which are α1 receptor agonists

A
  1. Phenylephrine-
  2. Tetrahydrozoline and xylometazoline-nasal decongestant
  3. Midodrine-postural hypotension
  4. Metarminol-
  5. Mephenteramine
  6. Methoxamine
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12
Q

Phenylephrine

A

α1 (vasoconstriction) receptor agonist

  1. Treatment of anaesthetic agent induced hypotension
  2. Mydriatic
  3. Nasal decongestant (like xylometazoline and tetrahydrozoline)
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13
Q

Xylometazoline and tetrahydrozoline

A

α1 (vasoconstriction) receptor agonist like phenylephrine

Nasal decongestant

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14
Q

Midodrine

A

α1 (vasoconstriction) receptor agonist like phenylephrine, xylometazoline and tetrahydrozoline

DoC for postural hypotension

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15
Q

Metarminol

A

α1 receptor agonist like phenylephrine,…

Treatment of hypotension caused by spinal anaesthesia

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16
Q

Mephenteramine

A

α1 receptor agonist like phenylephrine,…

Treatment of hypotension caused by arrhythmia

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17
Q

Methoxamine

A

α1 receptor agonist like phenylephrine,…

Treatment of shock

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18
Q

Examples of α2 receptor agonist

A

These drugs decrease bp and have sedative effect

  1. Clonidine
  2. Dexmedetomidine: pre anaesthetic agent
  3. Apraclonidine and Brimonidine: glaucoma
  4. Tizanidine: muscle relaxant
  5. Lofexidine: opioid dependence
  6. Moxonidine and Rilmenidine
  7. α-methyl DOPA
  8. Guanfacine and Guanabenz: ADHD,..
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19
Q

Clonidine

A

α2 receptor agonist

  1. DoC in treatment of hypertensive emergency
  2. DoC in tics associated with mild and moderate Taurette’s syndrome (otherwise Haloperidol)
  3. ADHD
  4. Prophylaxis of migraine
  5. Treating hot flashes
  6. Treating dependence of smoking, alcohol and opioids
  7. Diarrhoea associated with DM
  8. Used for pre anaesthetic medication
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20
Q

Side effects of clonidine

A 
α2 receptor agonist 
Withdrawal hypotension (treated by IV phentolamine)
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21
Q

Dexmedetomidine

A 
α2 receptor agonist like clonidine but highly potent
Used as a pre anaesthetic agent
1. Sedation 
2. Analgesia 
3. Decreased secretions
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22
Q

Apraclonidine and Brimonidine

A

α2 receptor agonist

Treating glaucoma

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23
Q

Tizanidine

A

α2 receptor agonist

Used as a muscle relaxant in disorders like ALS (Amyotrophic lateral sclerosis)

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24
Q

Lofexidine

A

α2 receptor agonist

Treating opioid dependence

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25
Q

Moxonidine and Rilmenidine

A

Imidazole receptor (decreases bp), α2 receptor agonist
Uses:
1. Resistant hypertension in elderly
2. Treating neuropathic pain

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26
Q

Methyl dopa

A

Prodrug which is converted into α-methyl NE
α2 receptor agonist and NE depletor
Treating PIH (pregnancy induced hypertension)
The DoC for PIH is oral labetalol
Side effect:
Haemolysis

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27
Q

Guanabenz

Guanfacine

A

α2 receptor agonist
Both are used in treating ADHD
Guanfenacine is the DoC for treating tics associated with Taurette’s syndrome (along with clonidine)

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28
Q

Mirabegron

A

β3 agonist
Used in urge incontenence
Under trial for treatment of CHF

Side effects:

  1. Decrease bp
  2. Head ache
  3. UTI
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29
Q

SABA examples

A

Short acting β2 agonists
Duration: 2-4 hours

Terbutaline-subcutaneous
Pirbuterol - inhalation
Albuterol (Salbutamol)- inhalation
These drugs are fast acting (along with formoterol)

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30
Q

LABA

A

Long acting β2 agonists
Duration: 12 hours

Salmeterol-slow acting
Formoterol-fast acting
Given via inhalation

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31
Q

VLABA

A

Very long acting β2 agonists
Duration: 24 hours

Carmoterol
Indicaterol
Olodaterol
Vilanterol
Given via inhalation for COPD
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32
Q

Fast acting β2 agonists and their uses

A

The fast acting β2 agonists are SABAs and formoterol

There are used via inhalational route for the treatment of acute attacks of bronchial asthma

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33
Q

Uses of LABA

A
  1. Prophylaxis of bronchial asthma
  2. Prophylaxis of exercise induced asthma
  3. With ICS for persistent bronchial asthma
  4. Along with anticholinergics for COPD
  5. Nocturnal asthma
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34
Q

The GINA (global initiative for asthma) guidelines

A 
Age:
0-5 years: SABA
6-11 years: SABA+ICS
>11 years: ICS+ Formoterol (ToC) 
 (if not then SABA+ICS)
ICS decreases the severity of exacerbation of bronchial asthma
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35
Q

Side effects of β2 agonists

A
  1. Tremors (most common)
  2. Palpitations
  3. Potassium levels:
    Open K+ channels ➡️ transient hyperkalemia
    Increases insulin ➡️ hypokalemia
    So used in treatment of hyperkalemia
  4. Hyperglycaemia
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36
Q

Tyramine

A

NE depletor
Dietary amine
Present in cheese and red wine
Can cause cheese reaction

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37
Q

Cheese reaction

A

Patient on MAO blockers (anti depressants) consumes wine or cheese ➡️ tyramine Increases ➡️ NE released into synapse ➡️ stimulates α1 receptors ➡️ hypertensive emergency

DoC: IV Phentolamine (α1 receptor blocker)

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38
Q

NE depletors

A
  1. Tyramine : cheese reaction
  2. Ephedrine (…) and Pseudoephedrine (nasal decongestant)
  3. Norephedrine: was used for obesity
  4. Methylphenidate
  5. Amphetamine and dextroamphetamine
  6. Guanedrel and Guanethidine
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39
Q

Ephedrine

A
  1. NE depletor
  2. Agonist of α and β receptor
    So mixed acting sympathomimetic
  3. DoC of hypotension in:
    pregnancy
    anaesthetic agents
  4. Mydriatic
  5. Nasal decongestant (along with it’s derivative pseudoephedrine)
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40
Q

Phenyl propanolamine or norephedrine

A

NE depletor
Was used for treatment of obesity
Now banned because associated with stroke

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41
Q

Methylphenidate

A

NE depletor and stimulant
Uses:
1. DoC for ADHD with 2 exceptions where the DoC is Atomoxetine
2. In narcolepsy where the DoC is Modafinil

42
Q

Use of a NE depletor in ADHD

A

Methylphenidate is the DoC in ADHD except in:

  1. ADHD with Tourette’s syndrome where it worsens tics
  2. ADHD with family history of drug abuse due to risk of drug abuse

In these two cases Atomoxetine (an anti depressant which is a NE reuptake inhibitor)

43
Q

Modafinil

A

DoC for:

  1. Narcolepsy (Solriamfetol, a DNRI -dopamine NE reuptake inhibitor, can also be used)
  2. Shift workers disease
  3. Sleepiness associated with OSA -obstructive sleep apnea
44
Q

Amphetamines

A 
NE depletor and Stimulant
So is used are similar to methylphenidate:
1. ADHD
2. Narcolepsy
3. Obesity because it causes anorexia

It’s derivative dextroamphetamine is specific for central action so it is more preferred

45
Q

Methamphetamine

A

Drug of abuse

Also called Cristal meth

46
Q

Why are amphetamines contraindicated in pregnancy

A

Amphetamines are teratogenic:

  1. IUGR
  2. Cardiac defect
  3. Cleft lip
  4. Biliary atresia
47
Q

Guanethidine and guanadrel

A

NE depletor
Can be used for hypertension
These are contraindicated in pheochromocytoma (because of initial sympathomimetic effect leading to a cheese reaction like situation)

48
Q

Anti glaucoma drugs

A
  1. Miotic agents: increase trabecular outflow
  2. Prostaglandin analogues: increases the uveoscleral outflow
  3. Sympathomimetics
  4. β blockers (selective or non-selective): decrease aqueous production
  5. CA inhibitors
49
Q

Miotic agents as anti glaucoma drugs

A

Miotic agents like pilocarpine, physostigmine, echothiophate, carbochol used in closed (and open) angle glaucoma to increase trabecular outflow
Stimulate M3 receptors

DoC for closed angle is pilocarpine

50
Q

Side effects of using miotic agents as anti glaucoma drugs

A

Stimulates M3 receptors

  1. Ciliary body or accommodation spasm
  2. Induced myopia
  3. Retinal detachment
  4. Corneal oedema
  5. ACHE inhibitors like physostigmine and echothiophate when given typically cause cataract (so contraindicated in phacic patients)
  6. Echothiophate can cause iris cysts or NLD obstruction
51
Q

Prostaglandin analogues and glaucoma

A

Latanoprost, Bimatoprost, Travoprost are PGF2α analogues
Increases the uveoscleral outflow
Given OD topically at night
DoC for open angle and normal tension glaucoma

52
Q

Side effects of prostaglandin analogues

A

P. Pigmentation of iris or (heterochromia iridis), eyebrow and periorbital skin (increases effect of tyrosinase)
C. Cystoid macular oedema (careful in DM)
O. Overgrowth of eyelashes (trichomegaly): so bimatoprost is used in hypotrichosis (anti cancer drug)
S. Sandy or dry eyes

53
Q

Contraindications of prostaglandin used as anti glaucoma drugs

A

Contraindicated in patients with:

  1. Uveitis
  2. Herpetic keratitis
54
Q

Sympathomimetics used as anti glaucoma drugs

A
  1. Epinephrine
  2. Dipivephrine (prodrug of epinephrine)
  3. α2 agonists like apraclonidine and ovimonidine
    Used via topical route for open angle glaucoma
55
Q

Mechanism of anti glaucoma action of sympathomimetics

A

1° mechanism of action is decreased aqueous production

2° mechanism of action increased uveoscleral outflow

56
Q

Side effects of sympathomimetic used as anti glaucoma drugs

A
  1. Common side effect is ocular allergy
  2. Epinephrine and Dipivephrine cause conjunctival pigmentation
  3. Apraclonidine-(α1 and) α2 agonist:
    α1 stimulation ➡️ mydriasis, lid retraction, conjunctival blanching
  4. Brimonidine α2 agonist which crosses BBB so:
    sedation, drowsiness and fatigue
    apnea in neonates
    dry mouth, hypertension
57
Q

β blockers as anti glaucoma drugs, examples

A 
Non selective β blockers like:
Timolol (most potent)
Levobunolol
Metipranolol
Carteolol
And selective β blockers like Betaxolol (longest acting)
58
Q

How β blockers act as anti glaucoma drugs

When are they used

A

Decrease aqueous production

2nd line drug for open angle glaucoma after latanaprost,…

59
Q

Side effects of β blockers as anti glaucoma drugs

A
  1. Contraindicated with systemic β blockers
  2. Contraindicated with patients with bronchial asthma or COPD, esp non selective β blockers
  3. Timolol can cause NLD obstruction and ocular cicatricial penphigoidnd
  4. Metripranolol can cause granulomatous anterior uveitis
60
Q

CA inhibitors used as anti glaucoma drugs

A 
1. Systemic drugs - acetazolamide:
 Oral or IV
 For acute congestive glaucoma 
2. Topical drugs - 
Brinzolamide, Dorzolamide
 For open angle glaucoma
61
Q

Side effects of CA inhibitors as anti glaucoma drugs

A

Systemic (acetazolamide):

  1. Metabolic acidosis
  2. Hypokalemia
  3. Hyperammonemia
  4. Nephrolithiasis

Local (Brinzolamide, Dorzolamide):

  1. Transient myopia
  2. Periorbital dermatitis
  3. Corneal oedema
62
Q

Netarsudil

A

Approved recently
Rho kinase inhibitor➡️ increases trabecular outflow
For treatment of open angle glaucoma
Latanaprost and Netarsudil fixed combination

63
Q

Sympatholytic drug classification

A 
A. α-receptor blockers:
 1. Non selective    
  (reversible and irreversible) 
 2. Selective
B. β-receptor blockers
64
Q

Tolazoline

A 
Reversible, non-selective α receptor blocker 
Peripheral vasodilator
Used in:
1. Raynaud’s disease
2. Vasodilator in angiography
65
Q

Phentolamine

A

Reversible, non-selective α receptor blocker
DoC in:
1. Clonidine withdrawal hypertension
2. Cheese reaction
3. Intraoperative HTN in pheochromocytoma
Used in:
1. Treating erectile dysfunction

66
Q

Drugs used in erectile dysfunction

A 
Phentolamine pyar
Bremelanolatide bhi
Naltrexone nahi
Ketanserin kar
S. Sildenafil (DoC)
A. Alprostadil
K. 
T. Trazodone
A. AlVIPtadil
67
Q

Bremenelotide

A

Melanocortin peptide receptor agonist
1. α-MSH melanocortin ➡️ MC1R ➡️ pigmentation
2. ACTH ➡️ MC2R
3. Miscellaneous ➡️ MC3,4,5R ➡️ central sexual arousal
treatment of HSDD, erectile dysfunction

68
Q

Phenoxybenzamine

A

Irreversible non-selective α-receptor blocker

DoC for preoperative HTN in pheochromocytoma

69
Q

Treatment of choice for pheochromocytoma

A

α-blockers followed by β-blockers to avoid HTN emergency

70
Q

Subtypes of α1 receptors

Significance

A

α1a: prostatic urethra, iris
α1b: blood vessels
α1d: blood vessels

71
Q

Non-selective α1 blockers

Uses

A
  1. Vasodilation and prostatic urethra dilation
  2. They increase HDL and decrease LDL
    DoC for:
  3. Benign prostatic hyperplasia and HTN.
    But the vasodilation is non selective (veins also dilated) ➡️ postural hypotension (1st dose effect) ➡️ night time dosing.
  4. HTN with dyslipidemia
72
Q

Non selective α1 blockers

Examples

A
  1. Terazosin
  2. Doxazosin
  3. Prazosin- Scorpion bite induced HTN or pulmonary oedema
  4. Alfuzodin-BPH
    Drugs used for HTN:
  5. Bunozosin
  6. Inforamin
  7. Urapidil
73
Q

Scorpion bite pharmacological treatment

A 
Prazosin: 
 Non selective α1 blockers
 Scorpion bite induced HTN or pulmonary oedema
Midazolone: CNS excitation
Atropine: bradycardia
74
Q

DoC for HTN with BPH or dyslipidemia

Examples:

A

Non selective α1 blockers

  1. Terazosin
  2. Doxazosin
  3. Prazosin (scorpion bite)
75
Q

Selective α1 blockers (α1a blockers)

A

Silodosin
Tamsulosin-most selective
DoC for BPH benign prostatic hyperplasia

76
Q

Side effects of α1 blockers

A

Prostatic urethra block ➡️ ejaculation abnormalities
Floppy iris
Side effects are maximum in tamsulosin
They are more in α1a blockers

77
Q

Uses of β blockers

A
  1. 2nd line drug for hyperreninemic HTN
  2. Prophylaxis of migraine
  3. Hyperthyroidism
  4. Anxiety
  5. Stable angina
    Propranolol is DoC for the above 4 conditions if they occur with HTN
  6. Chronic CHF
  7. History of MI
  8. DoC for HOCM (digoxin is CI)
  9. DoC for aortic dissection
  10. Glaucoma
78
Q

Non-selective β blockers

A

First generation β blockers

Blocks β1 and β2 receptors

79
Q

Effects of non-selective β blockers/first generation β blockers
(and hence CI in)

A

Blocks:

  1. Bronchodilation (bronchial asthma)
  2. Vasodilation (Raynaud’s disease,variant angina)
  3. Symptoms of hypoglycaemia except sweating (DM)
  4. Glycogenolysis and gluconeogenesis in skeletal muscle-decreased muscle capacity
80
Q

Selective β blockers

A

Block β1 only, less side effects

  1. Propranolol
  2. Oxprenolol
  3. Pindolol
  4. Timolol
  5. Nadolol
81
Q

Cardioselective β blockers

A 
Blocks β1 >> β2
My. Metoprolol
B. Bisoprolol, ‘Betaxolol’
E. Esmolol
T. aTenolol
A. Acebutolol
O. 
N. ‘Nebivolol’-most cardioselective
C. ‘Celiprolol’
E. 
‘These 3 are’ 3rd generation
Remaining are 2nd generation
82
Q

Third generation β blockers

A 
Cardioselective 
or 
(non cardioselective + vasodilation effect) β1 blocker
83
Q

Third generation β blocker with α1 blocking action

A

Labetolol
Carvedolol
Bevantolol
Bucindolol

84
Q

Features of carvedilol

A 
Third generation β1 blocker with α1 blocking action
Calcium channel blocker 
Antioxidant (like Nebivolol)
Anti inflammatory
Blocks LDL oxidation
85
Q

β1 blocker and β2 agonist

A

Bopindolol

86
Q

Third generation β blocker which increases the release of NO

A

N. Nipradilol

N. Nebivolol (antioxidant)- most cardioselective

87
Q

Third generation β blocker with K+ channel opening activity

A

Tilisolol

88
Q

β blockers which are partial agonist and intrinsic sympathomimetic effect
Examples

A

C. Celiprolol (cardioselective), Carteolol
L. Labetolol
A. Acebutolol (cardioselective)
P. Pindolol (maximum intrinsic sympathomimetic effect), Penbutolol

89
Q

β blockers which are partial agonist and intrinsic sympathomimetic effect
Properties

A
  1. Less bradycardia
  2. Not used in:
    migraine prophylaxis
    MI
90
Q

β blockers which are Na+ channel blockers and has local anaesthetic and membrane stabilising effect
Examples

A

Can. Carvedilol (max Na+ channel blocking action)
Blow. Betaxolol (min … effect, cardioselective)
L. Labetolol
A. Acebutolol (cardioselective)
M. Metoprolol
P. Pindolol, Propranolol (max Na+ channel blocking action)

91
Q

β blockers which are Na+ channel blockers and has local anaesthetic and membrane stabilising effect
Properties

A

Not used as topical agents against glaucoma (except cardioselective Betaxolol)
Due to their anaesthetic effect

92
Q

Water soluble β blocker

Properties

A

CI in renal failure

Do not cross BBB, no central side effects like insomnia, depression or nightmares

93
Q

Water soluble β blockers examples

A 
B. Betaxolol (cardioselective, bisoprolol
A. Atenolol (cardioselective)
N. Nadolol 
A. 
N. Nebivolol (most cardioselective)
A. Acebutolol (cardio selective)
S. Sotalol
Chips-Celiprolol (cardioselective)
94
Q

Longest acting β blocker

A

Nadolol

Water soluble selective first generation β blocker

95
Q

Shortest acting β blocker

Uses

A

Esmolol
2nd generation cardioselective β blocker metabolised by esterase of RBCs
Used in:
1. Emergency in PVST (paraoxysmal supraventricular tachycardia)
2. Intraoperative use

96
Q

β blocker with maximum plasma protein binding

A

Carvedilol

  1. Third generation β blockers
  2. Na+ channel blockers and has local anaesthetic and membrane stabilising effect
  3. α1 blocking action
  4. Calcium channel blocker
  5. Antioxidant (like Nebivolol)
  6. Anti inflammatory
  7. Blocks LDL oxidation
  8. Minimum bioavailability
97
Q

β protein with minimum plasma protein binding

A

Celiprolol
3rd generation water soluble cardioselective β blocker
Has partial agonist and intrinsic sympathomimetic effect

98
Q

β blockers with maximum (100%) bioavailability

A 
Penbutolol
Pindolol (1st generation selective β blocker)
Both these drugs partial agonist and intrinsic sympathomimetic effect
99
Q

β blockers with minimum (30%) bioavailability

A 
Carvedilol
Propranolol (1st generation, max Na+ channel blocking, local anaesthetic and membrane stabilising effect)
100
Q

Metabolic effects of different generations of β blockers

A 
1. 1st generation: negative effect
 Increased insulin resistance
 Hyperglycaemic
 Increased LDL/HDL ratio
2. 2nd generation: neutral
3. 3rd generation: positive effect 
 Opposite of 1st generation

Pharmacology MBBS (19 decks)

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