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Flashcards in USMLE Gen Pharm Deck (426)
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1

Km: Definition

Km = Substrate at 0.5*Vmax
Km reflects the affinity of the enzyme for its substrate

2

Vmax indicates what?

Vmax is directly proportional to the enzyme concentration.

3

Relationship between Km and affinity

–The lower the Km, the higher the affinity
–Smaller Km means enzyme is saturated earlier, which means that small amounts of substrate are picked up by the enzyme.

4

Reading an inverse curve: Y–intercept equals ?

1/Vmax
The higher the Y–intercept the lower the Vmax

5

Reading an inverse curve: X–intercept equals ?

(1/–Km)
The further to the right the x–intercept, the greater the Km

6

Reading an inverse curve: Slope equals ?

Km/Vmax

7

Reading an inverse curve: Effect of a competitive inhibitor

X–intercept farther to the right, meaning Km is greater, because you need more substrate to get the same effect as the competitive inhibitor is hogging the enzyme.

The y–intercept is the same, meaning Vmax hasn't changed, because there isn't any more enzyme.


The slope is greater, because Km has increased while Vmax has stayed the same.

8

Reading an inverse curve: Effect of a noncompetitive inhibitor

The x–intercept is the same, meaning Km is the same, because the affinity for the enzyme hasn't changed, there's just less of it.


The y intercept has increased, meaning Vmax has decreased, because enzyme has been inactivated by the noncompetitive inhibitor

The slope is greater, because Vmax has decreased while Km has stayed the same.

9

Competitive inhibitor: Resemble substrate

Yes

10

Competitive inhibitor: Overcome by increased substrate?

Yes

11

Competitive inhibitor: Binds active site?

Yes

12

Competitive inhibitor: Effect on Vmax

Unchanged. The amount of enzyme has not changed.

13

Competitive inhibitor: Effect on Km

Increased. A lot more substrate needs to be available to seize the active sites.

14

Noncompetitive inhibitor: Resemble substrate?

No

15

Noncompetitive inhibitor: Overcome by increased substrate?

No

16

Noncompetitive inhibitor: Binds active site?

No

17

Noncompetitive inhibitor: Effect on Vmax

Decreased. Takes the enzyme out.

18

Noncompetitive inhibitor: Effect on Km

Unchanged. Does not change the affinity for the enzyme.

19

Volume of distribution: Abbreviation

Vd

20

Vd: Stands for what?

Volume of distribution

21

Volume of distribution: definition

Vd = (amount of drug in the body)/(plasma drug concentration)

22

Volume of distribution: What alters it?

Liver and kidney disease

23

Where are drugs with a low Vd distributed?

plasma

24

Where are drugs with a medium Vd distributed?

extracellular space

25

Where are drugs with a high Vd distributed?

tissues

26

Clearance: definition

(rate of elimination of drug)/(plasma drug concentration)

=Vd x Ke where Ke=elimination constant

27

Half life: definition

The time required to change the amount of drug in the body by 1/2 during elimination (or during a constant infusion).

28

What percentage of steady state is a drug at after: 1 half life

50%

29

What percentage of steady state is a drug at after: 2 half lives

75%

30

What percentage of steady state is a drug at after: 3 half lives

87.50%

31

What percentage of steady state is a drug at after: 3.3 half lives

90%

32

What percentage of steady state is a drug at after: 4 half lives

94%

33

How many half lives does it take for a drug to reach the following percentage of steady state: 50%

1 half life

34

How many half lives does it take for a drug to reach the following percentage of steady state: 75%

2 half lives

35

How many half lives does it take for a drug to reach the following percentage of steady state: 87.5%

3 half lives

36

How many half lives does it take for a drug to reach the following percentage of steady state: 90%

3.3 half lives

37

How many half lives does it take for a drug to reach the following percentage of steady state: 94%

4 half lives

38

Cp stands for what?

target plasma concentration

39

What is the abbreviation for target plasma concentration?

Cp

40

In pharmacology, what is F an abbreviation for?

Bioavailability

41

What is the abbreviation in pharmacology for bioavailability?

F

42

Loading dose: Definition

Loading dose = (Cp * Vd)/F (where Cp equals the target plasma concentration, Vd equals volume of distribution, and F equals bioavailability)

43

Maintenance dose: Definition

Maintenance dose = (Cp * CL)/F (where Cp is the target plasma concentration and CL is clearance and F is bioavailability)

44

Zero–order elimination: definition

Constant elimination over time regardless of drug.

45

How does Cp vary with time during zero–order elimination?

Cp decreases linearly with time.

46

Zero–order elimination: Drug examples

–Ethanol
–Phenytoin
–Aspirin (at high concentrations)

47

First–order elimination: definition

Rate of elimination is proportional to drug concentration

48

Zero–order elimination vs First–order elimination: Comparison

Zero–order: Constant amount of drug eliminated per unit time

1st–order: Constant fraction of drug eliminated per unit time

49

How does Cp vary with time during first–order elimination?

Cp decreases exponentially with time.

50

Urine: Which species get trapped in urine?

Ionized species

51

In what kind of environment is the following trapped?: Weak acids

Basic environments

52

In what kind of environment is the following trapped?: Weak bases

Acidic environments

53

In what kind of environment is the following digested?: Weak acids

Acidic environments (below pKa)

54

In what kind of environment is the following digested?: Weak bases

Basic environments (above pKa)

55

How do you treat an overdose of the following?: Weak acids

Bicarbonate

56

How do you treat an overdose of the following?: Weak bases

Ammonium chloride

57

Phase I metabolism: Processes

Cytochrome P450
–reduction
–oxidation
–hydrolysis

58

Phase II metabolism: Processes

Conjugation
–acetylation
–glucuronidation
–sulfation

59

Phase I metabolism: Metabolites

–slightly polar
–water–soluble
–often still active

60

Phase II metabolism: Metabolites

–very polar
–renally excreted
–inactive

61

What phase of metabolism do geriatric patients lose first?

Phase I

62

Effect on dose/effect curve of: competitive antagonist

Shifts curve to the right, decreasing potency and increasing EC50.

63

Effect on dose/effect curve of: noncompetitive antagonist

Shifts curve downward, decreasing efficacy

64

What is EC50?

Dose causing 50% of maximal effect

65

What is Kd?

Concentration of drug required to bind 50% of receptor sites

66

How many half lives does it take for a drug to reach the following percentage of steady state: 97%

5 half lives

67

What percentage of steady state is a drug at after: 5 half lives

97%

68

Effect on dose/effect curve: Spare receptors

The drug binding and drug effect are independent of each other with effect to the left of binding.

This means that EC50 is lower than Kd, so very little drug needs to bind to get 50% of the effect.

69

Effect on dose/effect curve: Partial agonist

–Lower maximal efficacy
–Potency independent (amount of dose to get to maximum effect)

70

Therapeutic Index: Definition

#ERROR!

71

Where are nicotinic receptors found?

Preganglionic synapses before:
–Cardiac and smooth muscle (Parasympathetic and Sympathetic)
–Gland cells (Parasympathetic and Sympathetic)
–Nerve terminals (Parasympathetic and Sympathetic)
–Renal vascular smooth muscle (Sympathetic)

Neuromuscular junctions for skeletal muscle

72

What is the neurotransmitter at Nictoinic receptors?

Acetylcholine

73

What is the neurotransmitter at Muscarinic receptors?

Acetylcholine

74

Where are muscarinic receptors found?

Parasympathetic end plates:
–Cardiac and smooth muscle
–Gland cells
–Nerve terminals

Sympathetic end plate:
–Sweat glands

75

Where are D1 receptors found?

Sympathetic:
Renal vascular smooth muscle

76

What type of G–protein is associated with the following receptor type?: alpha–1

Gq

77

What type of G–protein is associated with the following receptor type?: alpha–2

Gi

78

What type of G–protein is associated with the following receptor type?: beta–1

Gs

79

What type of G–protein is associated with the following receptor type?: beta–2

Gs

80

What type of G–protein is associated with the following receptor type?: M1

Gq

81

What type of G–protein is associated with the following receptor type?: M2

Gi

82

What type of G–protein is associated with the following receptor type?: M3

Gq

83

What type of G–protein is associated with the following receptor type?: D1

Gs

84

What type of G–protein is associated with the following receptor type?: D2

Gi

85

What type of G–protein is associated with the following receptor type?: H1

Gq

86

What type of G–protein is associated with the following receptor type?: H2

Gs

87

What type of G–protein is associated with the following receptor type?: V1

Gq

88

What type of G–protein is associated with the following receptor type?: V2

Gs

89

What types of receptors are associated with the following G–proteins: q

–alpha–1
–M1
–M3
–H1
–V1

90

What types of receptors are associated with the following G–proteins: i

–alpha–2
–M2
–D2

91

What types of receptors are associated with the following G–proteins: s

–beta–1
–beta–2
–D1
–H2
–V2

92

What are the major functions of the following receptor type: alpha–1

Increase vascular smooth muscle contraction

93

What are the major functions of the following receptor type: alpha–2

–Decrease sympathetic outflow
–Decrease insulin release

94

What are the major functions of the following receptor type: beta–1

–Increase heart rate
–Increase contractility
–Increase renin release
–Increase lipolysis
–Increase aqueous humor formation

95

What are the major functions of the following receptor type: beta–2

–Vasodilation
–Bronchodilation
–Increased glucagon release

96

What are the major functions of the following receptor type: M1

CNS

97

What are the major functions of the following receptor type: M2

Decrease heart rate

98

What are the major functions of the following receptor type: M3

Increase exocrine gland secretions

99

What are the major functions of the following receptor type: D1

Relax renal vascular smooth muscle

100

What are the major functions of the following receptor type: D2

Modulate transmitter release (especially in brain)

101

What are the major functions of the following receptor type: H1

–Increase nasal/bronchial mucus production
–Contraction of bronchioles
–Pruritus
–Pain

102

What are the major functions of the following receptor type: H2

Increased gastric acid secretion

103

What are the major functions of the following receptor type: V1

Increased vascular smooth muscle contraction

104

What are the major functions of the following receptor type: V2

–Increased water permeability and reabsorption in the collecting tubules of the kidney

105

Gq protein pathway

–Receptor stimulated
–Gq protein stimulates Phospholipase C
–Phospholipase C catalyzes the conversion of Lipids to PIP2
–PIP2 splits into IP3 and DAG

IP3 stimulates an increase in Calcium concentration

DAG activates Protein Kinase C

106

Gs protein pathway

–Receptor stimulated
–Gs protein stimulates Adenylylcyclase
–Adenylylcyclase
catalyzes conversion of ATP to cAMP
–cAMP activates Protein Kinase A

107

Gi protein pathway

–Receptor stimulated
–Gi protein inhibits Adenylylcyclase
–Decreases conversion of ATP to cAMP
–Decreased activation of Protein kinase A

108

Cholinergic pathway (presynaptic events to receptor)

1. Choline transported into presynaptic bulb
2. Acetyl–Coa joints with Choline–ChAT to form acetylcholine, and the two are taken up by a vesicle.
3. The vesicle joins with the cell membrane and ACh is exocytosed
4. ACh is released into the synapse
5. Acetylcholine joints with the Cholinoceptor or is degraded by AChE into Choline + Acetate

109

Hemicholinum: Action and mechanism

Inhibits cholinergic transmission

Mechanism: Inhibits transfer of choline into presynaptic bulb

110

Vesamicol: Action and mechanism

Inhibits cholinergic transmission

Mechanism: Inhibits uptake of ACh into a vesicle in the presynaptic bulb

111

Ca2+: Action on presynaptic vesicles

Stimulates exocytosis of neurotransmitters from presynaptic bulb

112

Botulinum: Action and mechanism

Inhibits cholinergic transmission

Mechanism: Inhibits exocytosis of neurotransmitters from presynaptic bulb

113

Noradrenergic pathway (presynaptic events to receptor)

1. Tyrosine is transferred into the presynaptic bulb
2. Tyrosine is converted into DOPA
3. DOPA is converted to Dopamine
4. Dopamine is converted to Norepinephrine and transferred into a vesicle
5. Norepinephrine is exocytosed from the presynaptic terminal
6. 3 possibilities happen
a. Norepinephrine binds to a beta adrenoreceptor.
b. Norepinephrine is reuptaken by the releasing neuron
c. Norepinephrine binds to an alpha–2 receptor on the releasing neuron
d. It diffuses away/is metabolized.

114

Metyrosine: Action and mechanism

Action: Inhibits noradrenergic transmission

Mechanism: Inhibits step where tyrosine is converted into DOPA

115

Reserpine: Action and mechanism

Action: Inhibits noradrenergic transmission

Mechanism: Prevents sequestration of norepinephrine into vesicles

116

Guanethidine: Action and mechanism

Action: Inhibits noradrenergic transmission

Mechanism: Inhibits exocytosis of Norepinephrine from presynaptic bulb

117

Amphetamine: Action and mechanism

Action: Stimulates noradrenergic transmission

Mechanism: Stimulates exocytosis of norepinephrine from presynaptic bulb

118

Tricyclic antidepressant: Mechanism

Decreases reuptake of norepinephrine from synaptic cleft into releasing neuron

119

Cocaine: Mechanism

Decreases reuptake of norepinephrine from synaptic cleft into releasing neuron

120

Angiotensin II: Effect on noradrenergic pre–synaptic neurons

Enhances release of NE

121

Cholinomimetics: Direct agonists

Bethanechol, Carbachol, Pilocarpine, Methacholine

122

Cholinomimetics: Indirect agonists

Neostigmine (AChE inhibitor), Pyridostigmine, Edrophonium, Physostigmine, Echothiophate

123

Use of: Bethanechol

Postoperative and neurogenic ileus and urinary retention

124

Use of: Carbachol

–Glaucoma
–pupillary contraction
–release of intraocular pressure

125

Use of: Pilocarpine

Potent stimulator of:
–Sweat
–Tears
–Saliva

126

Use of: Methacholine

Challenge test for diagnosis of asthma

127

Use of: Neostigmine

AChE inhibitor
–Postoperative/neurogenic ileus/urinary retetnion
–Myasthenia Gravis
–Reversal of neuromuscular junction blockade (postoperative)
–No CNS penetration

128

Use of: Pyridostigmine

–Myasthenia Gravis (increases strength)
–does penetrate CNS

129

Use of: Edrophonium

Diagnosis of myasthenia gravis (extremely short acting)

130

Use of: Physostigmine

–Glaucoma (crosses blood–brain barrier into CNS)
–Atropine overdose

131

Use of: Ecthiophate

–Glaucoma

132

Mechanism of indirect cholinomimetics

Increase endogenous ACh

133

Synonym for indirect cholinomimetics

Anticholinesterases

134

Synonym for anticholinesterases

indirect cholinomimetics

135

Bethanechol: mechanism

–Activates bowel and bladder smooth muscle
–Resistant to AChE

136

Carbachol: mechanism

–Contracts ciliary muscle of eye (open angle)
–Contracts Pupillary sphincter (narrow angle)
–Resistant to AChE

137

Methacholine: mechanism

Stimulates muscarinic receptors in airway when inhaled

138

Symptoms of cholinesterase inhibitor poisoning

DUMBBELS SAC

–Diarrhea
–Urination
–Miosis
–Bronchospasm
–Bradycardia
–Excitation of skeletal muscle and CNS
–Lacrimation
–Sweating
–Salivation
–Abdominal Cramping

139

Antidote to cholinesterase inhibitor poisoning

–Atropine (muscarinic antagonist) +
–Pralidoxime (chemical antagonist used to regenerate active cholinesterase)

140

Cholinesterase inhibitors

–Parathion
–Other organophosphates

141

Cholinoreceptor blockers

–Atropine (homatropine, tropicamide)
–Benztropine
–Scopolamine
–Ipratropium
–Methscoplamine (oxybutin, glycopyrrolate)

142

Cholinoreceptor blockers used to produce: mydriasis and cycloplegia

Atropine, homatropine, tropicamide

143

Cholinoreceptor blockers used for: Parkinson's disease

Benztropine

144

Cholinoreceptor blockers used for: Motion sickness

Scopolamine

145

Cholinoreceptor blockers used for: Obstructive pulmonary disease

Ipratropium

146

Cholinoreceptor blockers used for: Genitourinary problems

–Methscopolamine
–Oxybutin
–Glycopyrrolate

147

Application of: Atropine

Produce mydriasis and cycloplegia

148

Application of: Homatropine

Produce mydriasis and cycloplegia

149

Application of: Tropicamide

Produce mydriasis and cycloplegia

150

Application of: Benztropine

Parkinson's Disease

151

Application of: Scopolamine

Motion sickness

152

Application of: Ipratropium

Obstructive pulmonary diseases

153

Application of: Methscopolamine

–Reduce urgency in mild cystitis
–Reduce bladder spasms

154

Application of: Oxybutin

–Reduce urgency in mild cystitis
–Reduce bladder spasms

155

Application of: Glycopyrrolate

–Reduce urgency in mild cystitis
–Reduce bladder spasms

156

Glaucoma drugs: Categories

–alpha–agonists
–beta–blockers
–diuretics
–cholinomimetics
–prostaglandins

157

Glaucoma drugs – alpha agonists:

Epinephrine
Brimonidine

158

Which glaucoma drug should not be used in closed–angle glaucoma?

Epinephrine

159

Epinephrine: Mechanisms and side effects

–M:
––Increased outflow of aqueous humor
–E:
––Mydriasis
––Stinging
––Do not use in closed angle glaucoma

160

Brimonidine: Mechanisms and side effects

M: Decreased aqueous humor synthesis
E: No pupillary or vision changes

161

Glaucoma drugs – beta blockers:

Timolol
Betaxolol
Carteolol

162

Glaucoma drugs – beta blockers: Mechanism and side effects

M: Decreased aqueous humor secretion
E: No pupillary or vision changes

163

Glaucoma drugs – diuretics: Drugs

Acetazolamide

164

Glaucoma drugs – diuretics: mechanisms and side effects

M: Decreased aqueous humor secretion due to decreased bicarbonate (via inhibition of carbonic anhydrase)

E: No pupillary or vision changes

165

Glaucoma drugs – Cholinomimetics: Drugs

Direct: Pilocarpine, Carbechol

Indirect: Physostigmine, Ecthiopate

166

Glaucoma drugs – Cholinomimetics: Mechanism and Side effects

M:
–Increase outflow of aqueous humor
–Contract ciliary muscle and open trabecular meshwork
–Use pilocarpine in emergencies
–Very effective at opening canal of Schlemm

E:
–Miosis
–Cyclospasm

167

Glaucoma drugs – Prostaglandins: Drugs

Latanoprost (PGF–2alpha)

168

Glaucoma drugs – Prostaglandins: Mechanism and Effects

M: Increase outflow of aqueous humor

E: Darkens color of iris (browning)

169

Atropine: General effects mnemonic

Blocks BUMBLED ASS

B: Bradycardia
U: Urination
M: Miosis
B: Bronchospasm
L: Lacrimation
E: Excitation of skeletal muscle and CNS
D: Diarrhea
A: Abdominal cramping
S: Sweating
S: Salivation

170

Atropine: Side effects

–Hot as a hare (Increased body temperature; hyperthermia in infants)
–Dry as a bone (Dry mouth and dry skin; Urinary retention in men with prostatic hypertrophy; Constipation)
–Red as a beet (Flushed skin)
–Blind as a bat (Cycloplegia, Acute angle–closure glaucoma in elderly)
–Mad as a hatter (disorientation)

171

Atropine: Mechanism

Muscarinic antagonist

172

Atropine: Effects on organ system: Eye

–Increased pupil dilation
–Cycloplegia

173

Atropine: Effects on organ system: Airway

–Decreased secretions

174

Atropine: Effects on organ system: Stomach

–Decreased acid secretion

175

Atropine: Effects on organ system: Gut

–Decreased motility

176

Atropine: Effects on organ system: Bladder

–Decreased urgency in cystitis

177

Hexamethonium: Mechanism

Nicotinic ACh receptor antagonist: Ganglionic blocker

178

Hexamethonium: Clinical use

Prevents vagal reflex responses to changes in blood pressure (eg prevents reflex bradycardia caused by NE)

179

Sympathomimetics: Catecholamines: List

–Epinephrine
–Norepinephrine
–Isoproterenol
–Dopamine
–Dobutamine

180

Sympathomimetics: Non–catecholamines: List

–Amphetamine
–Ephedrine
–Phenylephrine
–Albuterol
–terbutaline
–Cocaine
–Clonidine
–Alpha–methyldopa

181

Catecholamines: Epinephrine: Mechanism/selectivity

–alpha–1
–alpha–2
–beta–1 (low doses beta–1 selective)
–beta–2

182

Catecholamines: Epinephrine: Applications

–Anaphylaxis
–Glaucoma (open angle)
–Asthma
–Hypotension

183

Catecholamines: Norepinephrine: Mechanism/selectivity

More selective
–alpha–1
–alpha–2

Less selective
–beta–1

184

Catecholamines: Norepinephrine: Applications

Hypotension (but decreased renal perfusion)

185

Catecholamines: Isoproterenol: Mechanism/selectivity

beta–1 = beta–2

186

Catecholamines: Isoproterenol: Applications

AV block (rare)

187

Catecholamines: Dopamine: Mechanism/selectivity

In decreasing order:
–D1=D2
–beta
–alpha

188

Catecholamines: Dopamine: Applications

–Shock (Increased renal perfusion)
–Heart failure

189

Catecholamines: Dobutamine: Mechanism/selectivity

In decreasing order:
–Beta–1
–Beta–2

190

Catecholamines: Dobutamine: Applications

–Shock
–Heart failure cardiac stress testing

191

Catecholamines: Amphetamine: Mechanism/selectivity

–Indirect general agonist
–Releases stored catecholamines

192

Non–catecholamine sympathomimetics: Amphetamine: Applications

–Narcolepsy
–Obesity
–ADD

193

Non–catecholamine sympathomimetics: Ephedrine: Mechanism/selectivity

–Indirect general agonist
–releases stored catecholamines

194

Non–catecholamine sympathomimetics: Ephedrine: Applications

–Nasal decongestion
–Urinary incontinence
–Hypotension

195

Non–catecholamine sympathomimetics: Phenyephrine: Mechanism/selectivity

alpha–1 more than alpha–2

196

Non–catecholamine sympathomimetics: Phenyephrine: Applications

–Pupil dilator
–Vasoconstriction
–Nasal decongestion

197

Non–catecholamine sympathomimetics: Albuterol: Mechanism/selectivity

Beta–2 > Beta–1

198

Non–catecholamine sympathomimetics: Albuterol: Applications

Asthma

199

Non–catecholamine sympathomimetics: Terbutaline: Mechanism/selectivity

Beta–2 > Beta–1

200

Non–catecholamine sympathomimetics: Terbutaline: Applications

Asthma

201

Non–catecholamine sympathomimetics: Cocaine: Mechanism/selectivity

–Indirect general agonist
–Uptake inhibitor

202

Non–catecholamine sympathomimetics: Cocaine: Applications

–Vasoconstriction
–Local anesthesia

203

Non–catecholamine sympathomimetics: Clonidine: Mechanism/selectivity

–Centrally acting alpha–2 agonist
–Decreases central adrenergic outflow

204

Non–catecholamine sympathomimetics: alpha–methyldopa: Mechanism/selectivity

–Centrally acting alpha–2 agonist
–Decreases central adrenergic outflow

205

Non–catecholamine sympathomimetics: Clonidine: Applications

Hypertension (especially with renal disease, as there is no decrease in blood flow)

206

Non–catecholamine sympathomimetics: alpha–methyldopa: Applications

Hypertension (especially with renal disease, as there is no decrease in blood flow)

207

Sympathomimetics selective for: alpha–1

–Phenylephrine (alpha–1 more than alpha–2)
–Norepinephrine (alpha–1 and alpha–2 more than beta–1)

208

Sympathomimetics selective for: alpha–2

–Clonidine
–alpha–methyldopa
–Norepinephrine (alpha–1 and alpha–2 more than beta–1)
–Phenylephrine (alpha–1 more than alpha–2)
–Norepinephrine (alpha–1 and alpha–2 more than beta–1)

209

Sympathomimetics selective for: beta–1

–Dobutamine (beta–1 more than beta–2)
–Isoproterenol (beta–1 = beta–2)
–Epinephrine (at low doses)
–Albuterol, terbutaline (beta–2 more than beta–1)

210

Sympathomimetics selective for: beta–2

–Albuterol, terbutaline (beta–2 more than beta–1)
–Isoproterenol (beta–1 = beta–2)
–Dobutamine (beta–1 more than beta–2)

211

Sympathomimetics selective for: None (general agonists)

–Amphetamine
–Ephedrine
–Cocaine
–Epinephrine (alpha and beta)

212

Effect on blood pressure: Norepinephrine

Increases from 100 to 150

Mechanism:
1. Stimulates alpha more than beta
2. Systolic blood pressure goes up along with but more than diastolic blood pressure
3. Mean blood pressure rises

213

Effect on blood pressure: Epinephrine

Mean pressure stays at 100, with wide pulse–pressure (100)

Mechanism:
1. Nonselectively stimulates both alpha and beta receptors
2. Alpha receptors: Systolic blood pressure goes up
AND
beta receptors: Diastolic blood pressure goes down
3. Mean blood pressure stays the same
4. Pulse pressure is wide

214

Effect on blood pressure: Isoproterenol

Mean blood pressure goes down to 50, but pulse–pressure becomes wider (~75).

Mechanism:
1. Stimulates beta more than alpha.
2. Diastolic drops along with but more than systolic blood pressure
3. Mean blood pressure drops with wide pulse pressure

215

Effect on heart rate: Norepinephrine

1. Mean pressure goes up
2. Goes down to 50 (reflex bradycardia)

216

Effect on heart rate: Epinephrine

1. Beta–1 receptors are stimulated
2. Increases to 100

217

Effect on heart rate: Isoproterenol

1. Beta–1 receptors are stimulated more than alpha receptors
2. Increases to ~125

218

Sympathomimetic of choice for: Anaphylaxis

Epinephrine

219

Sympathomimetic of choice for: Open–angle glaucoma

Epinephrine

220

Sympathomimetic of choice for: Asthma

–Albuterol
–Terbutaline
–Epinephrine

221

Sympathomimetic of choice for: Hypotension

–Epinephrine
–Norepinephrine (though with decreased renal perfusion)
–Ephedrine

222

Sympathomimetic of choice for: AV block

Isoproterenol

223

Sympathomimetic of choice for: Shock

–Dopamine (increased renal perfusion)
–Dobutamine

224

Sympathomimetic of choice for: Heart failure

Dopamine

225

Sympathomimetic of choice for: Heart failure cardiac stress testing

Dobutamine

226

Sympathomimetic of choice for: Narcolepsy

Amphetamine

227

Sympathomimetic of choice for: Obesity

Amphetamine

228

Sympathomimetic of choice for: Attention defecit disorder

Amphetamine

229

Sympathomimetic of choice for: Nasal decongestion

–Ephedrine
–Phenylephrine

230

Sympathomimetic of choice for: Urinary incontinence

Ephedrine

231

Sympathomimetic of choice for: Dilation of pupils

Phenylephrine

232

Sympathomimetic of choice for: desired vasoconstriction

–Phenylephrine
–Cocaine

233

Sympathomimetic of choice for: Local anesthesia

Cocaine

234

Sympathomimetic of choice for: Treatment of hypertension

Clonidine and alpha–methyldopa (especially for those with renal disease, no decrease in blood flow to kidney)

235

alpha–blockers: drug list

Non–selective
–Irreversible: Phenoxybenzamine
–Reversible: Phentolamine
alpha–1 selective
–Prazosin
–Terazosin
–Doxazosin
alpha–2 selective
–Mirtazapine

236

Phenoxybenzamine: Mechanism

irreversible nonselective alpha–blocker

237

Phentolamine: Mechanism

reversible nonselective alpha–blocker

238

Prazosin: Mechanism

alpha–1 blocker

239

Terazosin: Mechanism

alpha–1 blocker

240

Doxazosin: Mechanism

alpha–1 blocker

241

Mirtazapine: Mechanism

alpha–2 blocker

242

Nonselective alpha blockers: Application

Pheochromocytoma

243

alpha–2 blockers: Application

Depression

244

alpha–1 blockers: Application

–Hypertension
–Urinary retention in BPH

245

Nonselective alpha blockers: Toxicity

–Orthostatic hypotension
–Reflex tachycardia

246

alpha–2 blockers: Toxicity

–Sedation
–Increase in serum cholesterol
–Increase in appetite

247

alpha–1 blockers: Toxicity

–1st–dose orthostatic hypotension
–dizziness
–headache

248

Which class of alpha blockers should you use for: Pheochromocytoma

Nonselective alpha blockers

249

Which class of alpha blockers should you use for: Hypertension

alpha–1 blockers

250

Which class of alpha blockers should you use for: Urinary retention in bph

alpha–1 blockers

251

Which class of alpha blockers should you use for: Depression

alpha–2 blockers (Mirtazapine)

252

beta–blockers: mechanism in control of: hypertension

–decreased cardiac output
–decreased renin secretion

253

beta–blockers: mechanism in control of: angina pectoris

1. decreased heart rate and contractility
2. result: decreased O2 consumption

254

beta–blockers: mechanism in control of: MI

decrease in mortality (no mechanism given)

255

beta–blockers: mechanism in control of: supraventricular tachycardia

decreased AV conduction velocity

256

beta–blockers: mechanism in control of: congestive heart failure

slows progression (no mechanism given)

257

beta–blockers: mechanism in control of: glaucoma

decreased secretion of aqueous humor

258

which beta–blockers are used in control of: supraventricular tachycardia

–Propranolol
–Esmolol

259

which beta–blockers are used in control of: glaucoma

Timolol

260

beta–blockers: toxicity: non–CV, non–CNS

–Impotence
–Asthma exacerbation

261

beta–blockers: toxicity: Cardiovascular

–bradycardia
–AV block
–congestive heart failure

262

beta–blockers: toxicity: CNS

–sedation
–sleep alterations

263

Non–selective beta blockers

–Propranol
–Timolol
–Nadolol
–Pindolol (partial agonist)
–Labetalol (partial agonist)

264

beta–1–selective beta–blockers

A BEAM of beta–1 blockers

–Acebutolol (partial agonist)
–Betaxolol
–Esmolol (short acting)
–Atenolol
–Metoprolol

265

Antidote for: Acetaminophen

N–acetylcysteine

266

Antidote for: Salicylates

1. Alkalinize urine
2. Dialysis

267

Antidote for: Anticholinesterases

–Atropine
–Pralidoxime

268

Antidote for: Organophosphates

–Atropine
–Pralidoxime

269

Antidote for: Anti–muscarinic anti–cholinergic agents

Physostigmine salicylate

270

Antidote for: beta–blockers

Glucagon

271

Antidote for: Digitalis

1. Stop digitalis
2. Normalize potassium
3. Lidocaine
4. anti–digitalis Fab fragments
5. Magnesium

272

Antidote for: Iron

Deferoxamine

273

Antidote for: Lead

1st line: CaEDTA & Dimercaprol
2nd line?: Penicillamine
Kids: Succimer
(First Aid lists Penicillamine in the antidotes section, but not in the section below, hence the ?)

274

Antidote for: Arsenic

–Dimercaprol (BAL)
–Succimer
–Penicillamine

275

Antidote for: Gold

–Dimercaprol (BAL)
–Succimer
–Penicillamine

276

Antidote for: Mercury

–Dimercaprol (BAL)
–Succimer

277

Antidote for: Copper

Penicillamine

278

Antidote for: Cyanide

–Nitrite
–Hydroxocobalamin
–Thiosulfate

279

Antidote for: Methemoglobin

Methylene blue

280

Antidote for: Carbon Monoxide

–100% Oxygen
–Hyperbaric Oxygen

281

Antidote for: Methanol

–Ethanol
–Dialysis
–Fomepizole

282

Antidote for: Ethylene glycol (antifreeze)

–Ethanol
–Dialysis
–Fomepizole

283

Antidote for: Opioids

Naloxone/naltrexone

284

Antidote for: Benzodiazepines

Flumazenil

285

Antidote for: Tricyclics

NaHCO3 (nonspecific)

286

Antidote for: Heparin

Protamine

287

Antidote for: Warfarin

–Vitamin K
–Fresh frozen plasma

288

Antidote for: tPA

Aminocaproic acid

289

Antidote for: streptokinase

Aminocaproic acid

290

For what drug(s) is the following an antidote?: N–acetylcysteine

Acetaminophen

291

For what drug(s) is the following an antidote?:
1. Alkalinize urine
2. Dialysis

Salicylates

292

For what drug(s) is the following an antidote?: Atropine

–Anticholinesterases
–Organophosphates

293

For what drug(s) is the following an antidote?: Pralidoxime

–Anticholinesterases
–Organophosphates

294

For what drug(s) is the following an antidote?: Physostigmine salicylate

Antimuscarinic, anticholinergic agents

295

For what drug(s) is the following an antidote?: Glucagon

beta–blockers

296

For what drug(s) is the following an antidote?: Deferoxamine

Iron

297

For what drug(s) is the following an antidote?: CaEDTA

Lead

298

For what drug(s) is the following an antidote?: Dimercaprol

Dimercaprol is GLAMorous

–Gold
–Lead
–Arsenic
–Mercury

299

For what drug(s) is the following an antidote?: Succimer

–Lead
–Arsenic
–Mercury
–Gold

300

For what drug(s) is the following an antidote?: Penicillamine

–Lead
–Copper
–Arsenic
–Gold

301

For what drug(s) is the following an antidote?: Nitrite

Cyanide

302

For what drug(s) is the following an antidote?: Hydroxocobalamin

Cyanide

303

For what drug(s) is the following an antidote?: Thiosulfate

Cyanide

304

For what drug(s) is the following an antidote?: Methylene blue

Methemoglobin

305

For what drug(s) is the following an antidote?: Oxygen

Carbon monoxide (Oxygen should be 100% or hyperbaric)

306

For what drug(s) is the following an antidote?: Ethanol

–Methanol
–Ethylene glycol (antifreeze)

307

For what drug(s) is the following an antidote?: Dialysis

–Methanol
–Ethylene glycol (antifreeze)
–Salicylates

308

For what drug(s) is the following an antidote?: Fomepizole

–Methanol
–Ethylene glycol (antifreeze)

309

For what drug(s) is the following an antidote?: Naloxone/Naltrexone

Opioids

310

For what drug(s) is the following an antidote?: Flumazenil

Benzodiazepines

311

For what drug(s) is the following an antidote?: NaHCO3

Tricyclic Antidepressants

312

For what drug(s) is the following an antidote?: Protamine

Heparin

313

For what drug(s) is the following an antidote?: Vitamin K

Warfarin

314

For what drug(s) is the following an antidote?: Fresh, frozen plasma

Warfarin

315

For what drug(s) is the following an antidote?: Aminocaproic acid

–tPA
–streptokinase

316

Lead poisoning: Signs and symptoms

LLEEAADD

–Lead Lines on:
––gingivae
––epiphyses of long bones on x–ray
–Encephalopathy
–Erythrocyte basophilic stippling
–Abdominal colic
–sideroblastic Anemia
–wrist Drop
–foot Drop

317

Lead poisoning: 1st line treatment for adults

Both:
–Dimercaprol
–EDTA

318

Lead poisoning: 1st line treatment for children

Succimer

(It "sucks" to be a kid who eats lead)

319

Causal agent for the following reaction: Atropine–like side effects

Tricyclic Antidepressants

320

Causal agent for the following reaction: Cardiac toxicity

–Doxorubicin (Adriamycin)
–Daunorubicin

321

Causal agent for the following reaction: Coronary vasospasm

Cocaine

322

Causal agent for the following reaction: Cutaneous flushing

–Niacin
–Ca2+–channel blockers
–Adenosine
–Vancomycin

323

Causal agent for the following reaction: Torsades des pointes

–Class III antiarrhythmics (sotalol)
–Class IA antiarrhytmics (quinidine)
–Cisapride

324

Causal agent for the following reaction: Agranulocytosis

–Clozapine
–Carbamazepine
–Colchicine

325

Causal agent for the following reaction: Aplastic anemia

–Chloramphenicol
–Benzene
–NSAIDs

326

Causal agent for the following reaction: Gray baby syndrome

Chloramphenicol

327

Causal agent for the following reaction: Hemolysis in G6PD–deficient patients

G6PD IS PAIN

–Isoniazid
–Sulfonamides
–Primaquine
–Aspirin
–Ibuprofen
–Nitrofurantoin

328

Causal agent for the following reaction: Thrombotic complications

oral contraceptive pills

329

Causal agent for the following reaction: Cough

ACE inhibitors (not ARBs)

330

Causal agent for the following reaction: Pulmonary fibrosis

–Bleomycin
–Amiodarone
–Busulfan

331

Causal agent for the following reaction: Acute cholestatic hepatitis

Macrolides

332

Causal agent for the following reaction: Focal to massive hepatic necrosis

–Halothane
–Valproic acid
–Acetaminophen
–Amanita phalloides

333

Causal agent for the following reaction: Hepatitis

INH

334

Causal agent for the following reaction: Pseudomembranous colitis

–Clindamycin
–Ampicillin

335

Causal agent for the following reaction: Adrenocortical insufficiency

Glucocorticoid withdrawal (HPA suppression)

336

Causal agent for the following reaction: Gynecomastia

Some Drugs Create Extra–Awesome Knockers

–Spironolactone
–Digitalis
–Cimetidine
–estrogens
–Alcohol (chronic use)
–Ketoconazole

337

Causal agent for the following reaction: Hot flashes

Tamoxifen

338

Causal agent for the following reaction: Gingival hyperplasia

Phenytoin

339

Causal agent for the following reaction: Osteoporosis

–Corticosteroids
–Heparin

340

Causal agent for the following reaction: Photosensitivity

SAT for a photo

–Sulfonamides
–Amiodarone
–Tetracycline

341

Causal agent for the following reaction: SLE–like syndrome

(It's not HIPP to have lupus)

–Hydralazine
–INH
–Procainamide
–Phenytoin

342

Causal agent for the following reaction: Tendonitis, tendon rupture, and cartilage damage

Fluoroquinolones (kids)

343

Causal agent for the following reaction: Fanconi's syndrome

Expired tetracycline

344

Causal agent for the following reaction: Interstitial nephritis

Methicillin

345

Causal agent for the following reaction: Hemorrhagic cystitis

–Cyclophosphamide
–Ifosfamide

346

Causal agent for the following reaction: Cinchonism

–Quinidine
–Quinine

347

Causal agent for the following reaction: Diabetes insipidus

–Lithium
–Demeclocycline

348

Causal agent for the following reaction: Seizures

–Bupropion
–Imipenem/cilastatin

349

Causal agent for the following reaction: Tardive dyskinesia

Antipsychotics

350

Causal agent for the following reaction: Disulfiram–like reaction

–Metronidazole
–Certain cephalosporins
–Procarbazine
–Sulfonylureas

351

Causal agent for the following reaction: Nephrotoxicity/neurotoxicity

Polymyxins

352

Causal agent for the following reaction: Nephrotoxicity/ototoxicity

–Aminoglycosides
–Loop diuretics
–Cisplatin

353

P–450 Inducers

Queen Barb takes Phen–phen and Strictly Refuses Greasy Carbs

–Quinidine (CYP3A4)
–Barbiturates
–Phenytoin
–St. John's Wort
–Rifampin
–Griseofulvin
–Carbamazepine

354

P–450 Inhibitors

Inhibitors Quickly Stop Cyber–Kids from Eating Grapefruit

–Isoniazid
–Quinidine (CYP2D6)
–Sulfonamides
–Cimetidine
–Ketoconazole
–Erythromycin
–Grapefruit juice

355

P–450 inducer or inhibitor: Quinidine

Inhibitor: CYP2D6 (more prominent)
Inducer: CYP3A4

356

P–450 inducer or inhibitor: Barbiturates

Inducer

357

P–450 inducer or inhibitor: Phenytoin

Inducer

358

P–450 inducer or inhibitor: Rifampin

Inducer

359

P–450 inducer or inhibitor: Griseofulvin

Inducer

360

P–450 inducer or inhibitor: Carbamazepine

Inducer

361

P–450 inducer or inhibitor: St. John's wort

Inducer

362

P–450 inducer or inhibitor: Isoniazid

Inhibitor

363

P–450 inducer or inhibitor: Sulfonamides

Inhibitor

364

P–450 inducer or inhibitor: Cimetidine

Inhibitor

365

P–450 inducer or inhibitor: Ketoconazole

Inhibitor

366

P–450 inducer or inhibitor: Erythromycin

Inhibitor

367

P–450 inducer or inhibitor: Grapefruit juice

Inhibitor

368

Active metabolite of ethylene glycol

Oxalic acid

369

Active metabolite of methanol

–Formaldehyde
–Formic acid

370

Active metabolite of ethanol

Acetaldehyde

371

Pathway and toxicities of metabolism of: ethylene glycol

1. Ethylene glycol is converted by alcohol dehydrogenase to
2. Oxalic acid causes:

–Acidosis
–Nephrotoxicity

372

Pathway and toxicities of metabolism of: methanol

1. Methanol is converted by alcohol dehydrogenase to
2. Formaldehyde and formic acid which cause:

–Severe Acidosis
–Retinal damage

373

Pathway and toxicities of metabolism of: ethanol

1. Ethanol is converted by alcohol dehydrogenase to
2. Acetaldehyde which causes:

–Nausea
–Vomiting
–Headache
–Hypotension

374

What enzyme is inhibited by disulfiram?

Acetaldehyde dehydrogenase

375

What inhibits acetaldehyde dehydrogenase?

Disulfiram

376

Clinical uses/toxicities for: Echinacea

Use: Common cold

Toxicities:
–GI distress
–dizziness
–headache

377

Clinical uses/toxicities for: Ephedra

Uses: As for ephedrine

Toxicities:
–CNS and cardiovascular stimulation
At high doses:
–Arrhythmias
–Stroke
–Seizure

378

Clinical uses/toxicities for: Feverfew

Use: Migraine

Toxicities:
–GI distress
–Mouth ulcers
–Antiplatelet actions

379

Clinical uses/toxicities for: Ginkgo

Use: Intermittent claudication

Toxicities:
–GI distress
–anxiety
–insomnia
–headache
–antiplatelet actions

380

Clinical uses/toxicities for: Kava

Use: Chronic anxiety

Toxicities:
–GI distress
–sedation
–ataxia
–hepatotoxicity
–phototoxicity
–dermatotoxicity

381

Clinical uses/toxicities for: Milk thistle

Use: Viral hepatitis

Toxicities: Loose stools

382

Clinical uses/toxicities for: Saw palmetto

Use: Benign prostatic hyperplasia

Toxicities:
–GI distress
–Decreased libido
–Hypertension

383

Clinical uses/toxicities for: St. John's wort

Use: Mild to moderate depression

Toxicities:
–GI distress and phototoxicity
–serotonin syndrome with SSRIs
–induces P–450 system

384

Clinical uses/toxicities for: DHEA

Uses: Symptomatic improvement in females with SLE or AIDS

Toxicities:
–Androgenization (premenopausal women)
–Estrogenic effects (post menopausal)
–Feminization (young men)

385

Clinical uses/toxicities for: Melatonin

Use:
–Jet lag
–Insomnia

Toxicities:
–Sedation
–Suppresses midcycle LH
–Hypoprolactinemia

386

Category for drug names ending with: –afil

Erectile dysfunction (eg Sildenafil)

387

Category for drug names ending with: –ane

Inhalational general anesthetic (eg Halothane)

388

Category for drug names ending with: –azepam

Benzodiazepine (eg Diazepam)

389

Category for drug names ending with: –azine

Phenothiazine (neuroleptic, antiemetic) (eg Chlorpromazine)

390

Category for drug names ending with: –azole

Antifungal (eg Ketoconazole)

391

Category for drug names ending with: –barbital

Barbiturate (eg Phenobarbital)

392

Category for drug names ending with: –caine

Local anesthetic (eg Lidocaine)

393

Category for drug names ending with: –cillin

Penicillin (eg Methicillin)

394

Category for drug names ending with: –cycline

Antibiotic, protein synthesis inhibitor (Tetracycline)

395

Category for drug names ending with: –ipramine

Tricyclic Antidepressant (eg Imipramine)

396

Category for drug names ending with: –navir

Protease inhibitor (eg Saquinavir)

397

Category for drug names ending with: –olol

beta–blocker (eg Propranolol)

398

Category for drug names ending with: –operidol

Butyrophone (neuroleptic) (eg Haloperidol)

399

Category for drug names ending with: –oxin

Cardiac glycoside (inotropic agent) (eg Digoxin)

400

Category for drug names ending with: –phylline

Methylxanthine (eg Theophylline)

401

Category for drug names ending with: –pril

ACE inhibitor (eg Captopril)

402

Category for drug names ending with: –terol

beta–2 agonist (eg Albuterol)

403

Category for drug names ending with: –tidine

H2 antagonist (eg Cimetidine)

404

Category for drug names ending with: –triptyline

Tricyclic antidepressant (eg Amitryptyline)

405

Category for drug names ending with: –tropin

Pituitary hormone (eg Somatotropin)

406

Category for drug names ending with: –zosin

alpha–1 antagonist (eg Prazosin)

407

Common ending for drug names in the following category: Erectile dysfunction

–afil (eg Slidenafil)

408

Common ending for drug names in the following category: Inhalational general anesthetic

–ane (eg Halothane)

409

Common ending for drug names in the following category: Benzodiazepine

–azepam (eg Diazepam)

410

Common ending for drug names in the following category: Phenothiazine (neuroleptic, antiemetic)

–azine (eg Chlorpromazine)

411

Common ending for drug names in the following category: Antifungal

–azole (eg Ketoconazole)

412

Common ending for drug names in the following category: Barbiturate

–barbital (eg Phenobarbital)

413

Common ending for drug names in the following category: Local anesthetic

–caine (eg Lidocaine)

414

Common ending for drug names in the following category: Penicillin

–cillin (eg Methicillin)

415

Common ending for drug names in the following category: Bacterial protein synthesis inhibitor

–cycline (eg Tetracycline)

416

Common ending for drug names in the following category: Tricyclic antidepressant

–ipramine (Imipramine)
–triptyline (Amitriptyline)

417

Common ending for drug names in the following category: Protease inhibitor

–navir (Saquinavir) (Mnemonic: Navir tease a pro)

418

Common ending for drug names in the following category: beta–antagonist

–olol (Propranolol)

419

Common ending for drug names in the following category: butyrophenone (neuroleptic)

–operidol (Haloperidol)

420

Common ending for drug names in the following category: Cardiac glycoside

–oxin (Digoxin)

421

Common ending for drug names in the following category: Methylxanthine

–phylline (eg Theophylline)

422

Common ending for drug names in the following category: ACE inhibitor

–pril (Captopril)

423

Common ending for drug names in the following category: beta–2 agonist

–terol (eg Albuterol)

424

Common ending for drug names in the following category: H2 antagonist

–tidine (eg Cimetidine)

425

Common ending for drug names in the following category: Pituitary hormone

–tropin (eg Somatotropin)

426

Common ending for drug names in the following category: alpha–1 antagonist

–zosin (eg Prazosin)