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Flashcards in Pharmacology 1 Deck (96)
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1
Q

Zero Order Elimination Drugs(4)

A

“PEA” ( a pea is round- shaped like the “0”)

  1. Phenytoin
  2. Ethanol (causes hangover!!)
  3. Aspirin(at high or toxic concentrations)
  4. cisplatin

Constant amount of drug elimination per unit time

2
Q
Weak acids(3) eliminated in urine
How treat overdoses?
A
  1. Phenobarbital
  2. Methotrexate
  3. Aspirin

Trapped in basic environment.
Treat overdose w/ Bicarbonate

3
Q
Weak bases(2) eliminated in urine
How treat overdoses?
A
  1. amphetamines
  2. TCAs

Trapped in acidic environment
Treat overdose w/ Ammonium chloride

4
Q

Notoriously slow Acetylators

Significance

A

Asians»White/Af. Am

increase drug concentration–> increase drug reactions

5
Q

Drugs with lower Therapeutic Index(4)

Whats the formula for Therapeutic Index?

A
  1. Digoxin
  2. Lithium
  3. Theophylline
  4. Warfarin (monitor PT/INR)

TI= ToxD50/ED50
(in animal studies= LD50/ED50)

6
Q

Diazepam is an agonist at GABA-R

What effect does Flumazenil have on the GABA receptor?

A

Competitive antagonist (resembles substrate)

  • decrease potency, no change in efficacy
  • can be overcome with increased concentration of agonist substrate
7
Q

NE is an agonist at alpha-R

What effect does phenoxybenzamine have on the alpha-R?

A

Noncompetitive antagonist

  • decrease efficacy
  • can’t be overcome by increased agonist substrate concentration
8
Q

Morphine is a full agonist at the u-R.

What effect does buprenorphine have on the u-R?

A

partial agonist

  • acts at same site as full agonist but with lower efficacy
9
Q
Sypathetic G-protein type:
a1
a2
B1
B2
B3
A
a1- q
a2-i
B1-s
B2-s
B3-s
10
Q
Parasympathetic G-protein type:
M1
M2
M3
What type of receptor is nAch-R
A

M1-q
M2-i
M3-q

nAch-R: ligand-gated Na/K channel (Nn and Nm)

11
Q

Dopamine G-protein type:
D1
D2

A

D1-s

D2-i

12
Q

Histamine G-protein type:
H1
H2

A

H1-q

H2-s

13
Q

Vasopressin G-protein type:
V1
V2

A

V1-q

V2-s

14
Q

Mnemonic for G-proteins

A

“After QISSeS(kisses), you get a QIQ(kick) out of SIQ(sick) SQS (super qinky sex)”

15
Q

Which receptors are Gs linked?

A

B1-3, D1, H2, V2

16
Q

Which receptors are Gi linked?

A

M2, a2, D2

“MAD 2’s”

17
Q

Which receptors are Gq linked?

A

H1, a1, V1, M1, M3

“HAVe 1 M&M”

18
Q

Hemicholium (experimental rat drug):

MOA

A

inhib choline transporter

prevent choline uptake into cholinergic axon

19
Q

Vesamicol(experimental rat drug):

MOA

A
inhib vAchT
(prevent Ach transport into vesicle in cholinergic axon terminal)
20
Q

Botulium:

MOA

A

inhib SNAP-25

prevent Ach vesicle fusion for NT release

21
Q

Metyrosine:

MOA

A

inhib tyrosine hydroxylase

prevent tyrosine–>DOPA

22
Q

Reserpine (anti-pysch):
MOA
Important adverse

A
Inhib VMAT 
(prevent Dopamine transport into Noradrenergic vesicle)
* decrease BP b/c prevents NE storage-->loose a1 vasoconstriction
23
Q

Bretylium & Guanethidine (never used):

MOA

A

inhib Noradrenergic vesicle fusion at synapse –> inhib NT release

24
Q

Amphetamine & ephedrine:

MOA

A

increase fusion of vesicles at Noradrenergic synapse–> increase release of all Monoamines

  • Amphetamines use NET to enter presynaptic terminal, and use the VMAT to enter vesicle. This displaces NE from vesicle. Once NE reaches threshold concentration w/in terminal–>reverse NET and NE is expelled into Synaptic Cleft contributing to increased NE observed
25
Q

Cocaine & TCAs & Amphetamine:

MOA

A

inhib reuptake transporter & inhib DA transporter

–>many monoamine’s reuptake inhibited–> Feel great and jacked up

26
Q

ACEi effect on adrenergic-R in axon

A

inhib AT-II binding to “Release-modulating receptors”

–>prevent release of monoamines

27
Q

Precursor to Tyramine (enzyme for conversion)
Enzyme which degrades Tyramine
Foods which contain Tyramine

A
  • Tyrosine–>tyramine via tyrosine decarboxylase
  • degraded by MAO
  • Cheese and Wine
28
Q

Describe D-D Tyramine & MAOi interaction

A
  1. Excess tyramine enters presynaptic vesicles and displaces other NTs
  2. increase active presynaptic NTs
  3. increase NT diffusion in cleft
  4. increase sympathetic stimulation
  5. –>HYPERTENSIVE CRISIS
29
Q
Buproprion:
MOA
Use (2)
Adverse(4)
Sexual effect?
A

-increase Ne/DA via unknown MOA
Uses: 1. depression 2. smoking cessation

  1. Tachycardia
  2. insomnia
  3. HA
  4. seizures in ANOREXICS
    * NO SEXUAL SIDE EFFECTS
30
Q
Describe the C. botulinum toxin:
type of toxin 
MOA
site of action
Where do adults get toxin
Where do babies get toxin
Antidote
A

-heat-labile toxin (protease) cleaves SNARE
-Toxin inhib Ach release at NMJ–>Flaccid paralysis
-Adults= inject preformed toxin
-Babies= ingest Honey spores–>Floppy Baby
Tx: Anti-toxin

31
Q

Can Dopamine cross BBB?

Can L-DOPA cross BBB?

A

No

Yes

32
Q

Direct Cholinergic agonists:

Name (4)

A
  1. BethaneCHOL
  2. CarboCHOL
  3. MethaCHOLine
  4. Pilocarpine
33
Q
Bethanechol:
Action
Effects 
Use (3)
ACHE effect
A

“Bethany, call me to activate bowels and bladder”

  1. Post-op ileum
  2. neurogenic ileus (common in DM)
  3. urinary retention
    - resistant to AchE
34
Q

Carbachol:
Description
Use (1)

A

CARBon copy of AcetylCHOLine

1. open-angle glaucoma (constricts pupil and relieves IOP)

35
Q

Methacholine:
MOA
Use (1)

A

Stimulates mAchR in airways when inhaled

1. Asthma challenge test (measure FEV1 and FVC)

36
Q

Pilocarpine:
MOA
ACHE effect
Use(4)

A
  • Contract CiliaryM. and pupillary Sphincter
  • resistant to AchE
    1. stim Sweat, tears, & saliva
    2. Open angle glaucoma (ciliary m.)
    3. Closed angle glaucoma (sphincter m.)
    4. Sjogrens (xerostomia)

“you cry, drool, and sweat on your PILOw”

37
Q

another term for anti cholinesterase

overall effect

A
  • indirect agonists

- increase Ach

38
Q

3 anticholinesterases used to treat Alzheimers

A
  1. Donepezil
  2. Galantamine
  3. Rivastigmine
39
Q

Edrophonium:
Use
Half-life

A

Diagnosis Myesthenia Gravis historically
(now diagnosed by anti-ache Ab test)
very short acting

40
Q

Neostigmine:
Use(3)
CNS penetration

A
  1. post-op/neurogenic ileum & urinary retention (like bethanachol
  2. Myasthenia gravis
  3. Reversal of NMJ blockade (post-op)

No CNS penetration (quaternary amine) “Neo CNS”

41
Q

Physostigmine:
Use
CNS penetration

A

“PHYsostigmine ‘PHYxes’ atropine overdose
1. Anticholinergic toxicity

CNS penetration (tertiary amine)

42
Q

Pyridostigmine:
Use
CNS penetration
Half-life

A

“PyRIDostiGMine gets RID of Myasthenia Gravis”
1. Myasthenia gravis (increase muscle strength)

No CNS penetration (quaternary amine)
Long-acting

43
Q

2 drugs used to treat Myasthenia Gravis

A
  1. NEOstiGMine
  2. PyRIDostiGMine
    (neither cross BBB)
44
Q

2 Contra/Caution for all cholinomimetic agents (both direct and indirect agonists)

A
  1. COPD/Asthma exacerbation

2. Peptic Ulcers (in susceptible patients)

45
Q

Symptoms of Cholinesterase inhibitor poisoning

Who is the typical patient on Boards? Typical cause?

A
Farmer with organophosphate poisoning like parathion
"DUMBBELSS"
Diarrhea/N
Urination
Miosis
Bronchospasm
Bradycardia
Excitation of Sk.Muscle/CNS
Lacrimation
Sweat
Salivation
-->Respiratory failure if untreated
46
Q

Antidote for cholinesterase inhibitor poisioning (2)

A
  1. atropine (competitive inhib)

2. pralidoxime (regenerates AchE if given early)

47
Q

3 drugs which produce Mydriasis and Cycloplegia

A
  1. atropine
  2. homatropine
  3. tropicamide
48
Q

Muscarinic antagonist to treat

Parkinson’s/ Acute dystonia

A

Benztropine

“park my Benz”

49
Q

2 uses for Glycopyrrolate

A

“‘GI’copyR(resp)rolate”

parenteral: pre-op reduction of airway secretions
oral: drooling and peptic ulcers

No cross BBB

50
Q

2 muscarinic antagonists to treat Irritable bowel Synd

A
  1. Hyoscyamine

2. Dicyclomine

51
Q

2 muscarinic antagonists to treat COPD/Asthma

A
  1. Ipratropium
  2. tiotropium

“TIO PRAys to breath”

52
Q

4 drugs to treat Overactive bladder/urge incontinence

A

” On the Darn Toilet, Sorry”

  1. Oxybutynin
  2. Trospium
  3. Darifenacin
  4. Tolterodine
  5. Solifenacin
53
Q

Drug to treat motion sickness

A

Scopolamine

54
Q
Atropine Effects:
Eye
Airway
Stomach
Gut
Bladder
A
dilate/cycloplegia
decrease secretions in airway
decrease stomach acid secretions
decrease GI motility
decrease urgency in cystitis
55
Q

Atropine:
Use
Adverse

A

Blocks DUMBBeLSS in cholinesterase inhib poisoning. DOES NOT BLOCK ‘E-EXCITATION OF SK.MUSCLE/CNS WHICH AR MEDIATED BY nACH-R

  1. Hot as a hare (M3)
  2. Dry as a bone (M3)
  3. Red as a beet (M3)
  4. Blind as a bat (M3)
  5. Mad as a hatter (M1 in CNS
56
Q

Atropine:

CONTRA (3)

A
  1. Elderly (can cause Closed angle glaucoma via mydriasis)
  2. Men with BPH (urinary retention)
  3. infants (hyperthermia)
57
Q

Effect of Jimson weed (Datura)

Chemicals causing effect (2)

A

Gardener’s pupil
MYDRIASIS due to plant alkaloids (ENLARGED FROM SPHINCTER PARALYSIS)

  1. scopolamine
  2. atropine
58
Q

Albuterol/ Salmeterol:
Receptor target
Use

A

B2>B1 (COPD/Asthma)
Albuterol (SABA)
Slmeterol (LABA)

59
Q

Dobutamine:
Receptor target
Use (2)

A

B1>B2, a

  1. HF (inotropic>chronotropic)
  2. cardiac stress testing
60
Q

Dopamine:
Receptor target
Use (3)
Dose dependent actions

A

D1=D2>B>a

  1. unstable bradycardia
  2. HF
  3. shock
Low dose (Beta)-->inotropic and chronotropic effects
High dose (alpha)-->vasoconstriction
61
Q

Epinephrine:
Receptor target
Use(3)
Dose dependent actions

A

B2/B1>a (methyl group addition from Ne–>Epi)

  1. Anaphylaxis
  2. Asthma
  3. Open-angle glaucoma

High dose–>alpha effect predominate

62
Q

Fenoldopam:
Receptor target
Use(4)
Potential adverse(2)

A

D1 (“FenolDOPAM”)

  1. post-op hypertension
  2. hyeprtensive crisis
  3. vasodiltor (coronary, peripheral, renal, and splanchnic)
  4. promote naturesis

Potentially cause hypotension and tachycardia

63
Q

Isoproterenol:
Receptor target
Use
potential adverse

A

B1=B2
1. electrophysiologic eval of tachyarrhythmias

potentially can worsen ischemia

64
Q

Midodrine:
Receptor target
Use(2)
potential adverse

A

a1

  1. autonomic insuff.
  2. postural hypotension

potentially exacerbate spine hypertension

65
Q

Norepinephrine:
Receptor target
Use(2)

A

a1»a2>B1

  1. hypotension
  2. septic shock
66
Q

Phenylephrine:
Receptor target
Use(3)

A

a1>a2

  1. hypotension (vasoconstriction)
  2. ocular procedures (mydriatic)
  3. rhinitis (decongestant)
67
Q

Amphetamine:
MOA(3)
Use (3)

A

Indirect general agonist, reuptake inhib, release stored catecholamines

  1. Narcolepsy
  2. obesity
  3. ADHD
68
Q

Cocaine:
MOA (2)
Use(1)

A

Indirect general agonist, reuptake inhib

  1. vasoconstrictor/ local anesthetic for Rhinoplasty
69
Q

Cocaine:
What should never be given if cocaine intoxication is suspected?
Why?

A

BB

–>can lead to unopposed a1 activation–>extreme HTN

70
Q

Ephedrine:
MOA(2)
Use (3)

A

indirect general agonist, releases stored catecholamines

  1. Nasal decongestion
  2. Urinary incontinence
  3. Hypotension
71
Q

Which dopamine receptor is generally in PNS?
CNS?

**exceptions to this rule do exist

A

PNS–> D1 (perpheral, coronary, renal, splanchnic circulations for widespread vasodilation)

CNS–>D2

72
Q

Low dose DA stimulates?

High dose DA stimulates?

A
low= D1 (vasodilation)
high= a1(vasoconstriction)
73
Q

Clonidine/ Guanfacine:
MOA
Use(3)
Adverse (5)

A

a2-agonist (Gi)
Use: 1. hypertensive urgency 2. ADHD 3. Tourette

Adverse:

  1. CNS depression
  2. Bradycardia
  3. Hypotension
  4. Resp depression
  5. Miosis
74
Q

alpha-methyldopa:
MOA
Use (1)
Adverse (2)

A

a2-agonist (Gi)
Use: HTN in pregnancy

Adverse:

  1. Direct Coombs (autoimmune hemolytic anemia)
  2. SLE-like syndrome (check anti-histone) (“Lupus is SHIPP-E, but not included)
75
Q

Effects of a2 stimulation

A

Sympatholytic:

  1. decrease SNS
  2. decrease insulin release
  3. decrease lipolysis
  4. decrease aqueous humor prod. in eye
  5. increase platelet aggregation
76
Q

Nonselective a-blockers:
Name (2)
which is reversible vs. irreversible?
Shared adverse (2)

A
  1. Phenoxybenzamine- irreversible
  2. Phentolamine- reversible
    “PhenTOLamine is TOLtally reversible”
  3. Orthostatic Hypotension
  4. Reflex tachycardia (via baroreceptors)
77
Q

Phenozybenzamine:
MOA
Use(1)

A

nonselective, irreversible a-blocker

  1. Pheochromocytoma (pre-op) to prevent Hypertensive crisis
    * classic question on boards!!!
78
Q

Phentolamine:
MOA
Use(1)

A

nonselective, reversible a-blocker
“PhenTOLamine is TOLtally reversible”

  1. Give to patient on MAOi’s who eats tyramine containing foods (prevent hypertensive crisis)
    * classic question on boards!!!
79
Q
Prazosin
Terazosin
Doxazosin
Tamsulosin:
MOA
Use (3)
Adverse(3)
A

a1 selective blockers (all end in ‘-osin’)

  1. BPH urinary symptoms
  2. PTSD (‘P’razosin)
  3. HTN (except tamsulosin

Adverse: 1. 1st dose orthostatic hypotension 2. Dizzy/HA

80
Q

Mirtazapine:
MOA
Use (1) & How
Adverse (3)

A

a2 selective blocker

Treat Depression
(no (-)feedback–> increase 5-HT/NE/DA release)

  1. sedation
  2. increase cholesterol
  3. increase appetite
81
Q

BBs:

Name (12)–>”-olol”

A
  1. Acebutolol (partial agonist)
  2. Atenolol
  3. Betaxolol
  4. Carvedilol
  5. Esmolol
  6. Labetalol
  7. Metoprolol
  8. Nadolol
  9. Nebivolol
  10. Pindolol (partial agonist)
  11. Propranolol
  12. Timolol
  • A-M= B1 selective
  • N-Z= B2 selective
  • Nonselective a and B antagonists have modified suffixes: CarvedILOL & LabetALOL
82
Q

BB effects on:
Angina Pectoralis
MI
HTN

A

Angina: decrease HR–>decrease O2 consumption
MI: decrease mortality
HTN: decrease CO & decrease Renin secretion via block of JGA cells (B1-R)

83
Q

BB:
2 drugs to treat SVT:
MOA

(supraventricular tachycardia)

A

Class II antiarrhythmics:

  1. metoprolol
  2. Esmolol

decrease AV conduction velocity

84
Q

BB:

3 drugs to treat Heart Failure

A
  1. Bisoprolol
  2. Carvediol
  3. Metoprolol

decrease mortalilty

85
Q

BB:
1 drug to treat glaucoma
MOA

A

Timolol (‘Timmy can BBarely see’)

decrease secretion of aqueous humor (B2=ciliary process)

86
Q

BB:
2 drugs for variceal bleeding
MOA(2)

A
  1. Nadolol
  2. Propranolol

decrease hepatic venous pressure gradient
decrease portal hypertension

87
Q

BB:

Adverse(4)

A
  1. Erectile dysfunction (not really true though)
  2. CV- bradycardia, AV block, HF
  3. CNS- seizures, sedation, sleep alterations
  4. dyslipidemia (metoprolol
  5. asthma/COPD exacerbations (Never use nonselective BB in these pts)
88
Q

BB:
2 Contraindications
Can diabetics use BB

A
  1. Cocaine use: risk of unopposed a-adrenergic agonist activity
  2. COPD/Asthma (nonselective BBs contra)

Despite theoretical concern of masking hypoglycemia in DM, benefits likely outweigh risks (NOT A CONTRA)

89
Q

BB:

2 drugs which are partial agonists

A
  1. acebutolol(B1 selective antagonist) (partial agonist)

2. pindolol (B2 selective antagonist) (partial agonist)

90
Q

BB–>Nebivolol:

MOA/Receptors involved

A

combines B1-block with B3-R stim –>increase NO release–>Sm. Muscle relaxes–> decrease TPR/Afterload

91
Q

Importance of B1 selective blocking?

A

cardio selective

decrease HR/contractility/CO/MVO2

92
Q

3 important varicies

2 BB drugs to treat vatical bleeding

A
  1. esophageal–> 30% chance of killing patient
  2. umbilical
  3. rectal

Tx: Propranolol, Nadolol

93
Q

3 Ingested Seafood toxins

A
  1. tetrodotoxin
  2. ciguatoxin
  3. Histamine from scombroid poisoning
94
Q
Tetrodotoxin:
geographic / source
Action
Symp (4)
Treatment
A
  • Japan/ pufferfish
  • highly potent, binds fast VGNa Channels in Cardiac/Nerve–>prevent depolarization
    1. N/D 2. Paresthesias 3 Dizzy 4. Weakness/Loss of Reflexes

Treat: supportive

95
Q
Ciguatoxin:
geographic
source(3)
Action
Symp 
Treatment
A
  • 20% foodborne toxin in USA
  • barracuda, snapper, moray eel
  • Opens Na+ channels–>depol in all memb
  • Symp: mimic Cholinergic poisoning (N/V/D/abd. pain after fish)

Treat: supportive

96
Q
Scamboid Poisoning: 
Source(4)
Action
Symp/ Misdiagnosis
Treatment
A
  • Spoiled dark-meat fish (tuna, mahi-mahi, mackerel, bonito)
  • histadine–>histamine via Bacterial histidine decarboxylase
    -symp mimic Anaphylaxis (misdiagnosed as fish allergy)
    (burning of mouth, flushing, erythema, urticaria, itching–>broncospasms/angioedema/hypotension

Treat: 1. Anti-histamines 2. Albuterol/Epi if needed