Pharm 1 - Pharmacokenetics/dynamics/ANS p232-246 Flashcards
(164 cards)
1
Q
A
2
Q
A
3
Q
How do competitive inhibitors affect Km?
A
Increase Km (dec affinity)
4
Q
The further to the right the x-intercept (ie, closer to zero), the greater the ___ and the lower ______.
A
The further to the right the x-intercept (ie, closer to zero), the greater the Km and the lower the affinity.
5
Q
Which type of inhibitor will cross x-intercept of an unihibited substrate?
What does that x-intercept represent?
A
non competitive inhibitor
X-intercept = 1/-Km
6
Q
What type of inhibitor will cross the y-intercept of an unihibited substrate? What is that y-intercept = to?
A
competitive inhibitor
y-intercept = 1/Vmax
7
Q
Competitive (-)’r of Diazepam? What is the rec’r?
A
Flumazenil
GABAA- R
8
Q
Competitive (-)’r vs organophosphates?
A
Atropine
9
Q
Competitive (-)’r of xanthine oxidase?
A
Allopurinol
10
Q
ex of competitive ACh antagonist
A
neuromuscular blocking drugs
Atracurium, cisatracurium, pancuronium, rocuronium, tubocurarine, vecuronium
11
Q
competitive aldosterone receptor antagonists in cortical collecting tubule?
A
Spironolactone, Eplerenone
12
Q
Competitive inhibitors of progestins at progesterone receptors?
A
Mifepristone, ulipristal.
13
Q
Nonsteroidal competitive inhibitor at androgen receptors? use?
A
Flutamide; Prostate carcinoma
14
Q
A
15
Q
How does competitive antagonists affect efficacy and potency?
A
dec potency; doesn’t change efficacy
16
Q
How does a non competitive antagonist affect potency and efficacy?
A
dec potency and efficacy
17
Q
How does partial agonist affect potency?
A
It doesn’t - it is independent of it.
18
Q
How does efficacy of a partial agonist compare vs a full agonist?
A
It has less efficacy than a full agonist
19
Q
A
20
Q
How to calc loading dose?
A
(Cp × Vd) / F
Cp - plasma conc
Vd - Vol of distribution
F = bioavail
21
Q
How to calc maintenance dose?
A
Maintenance dose =
(Cp × CL × τ )/ F
Cp = target plasma concentration at steady state
Cl = clearence τ = dosage interval (time between doses), if not administered continuousl
F = bioavail
22
Q
In renal or liver disease, maintenance dose ____ and loading dose is usually ______.
A
In renal or liver disease, maintenance dose Dec and loading dose is usually unchanged.
23
Q
Time to steady state depends primarily on _____ and is independent of ____ and _____ ________.
A
Time to steady state depends primarily on t1/2 and is independent of dose and dosing frequency.
24
Q
How to calc t1/2?
A
t1/2 = (0.7 × Vd)/Cl in first-order elimination
25
Drugs with narrow therapeutic index?
Warfarin, Theophylline, Digoxin, Lithium, anti-epitleptics
**War**ning, **Th**ese **D**rugs **a**re **lethal**
26
Two drugs with additive effects? What does that mean?
Effect of substance A and B together is equal to the sum of their individual effects
Aspirin and acetaminophen
27
Give ex of a drug that has a permissive effect on another? what does that mean?
Presence of substance A is required for the full effects of substance B
Cortisol has a permissive effect on catecholamines, as it upregulates α1-receptors on arterioles, making them more sensitive to Epi/NE (leading to inc BP)
28
Give ex of two synergistic drugs? define.
Effect of substance A and B together is greater than the sum of their individual effects
Clopidogrel with aspirin
29
What is a tachyphylactic drug interaction?
Acute decrease in response to a drug after initial/repeated administration
ex/
Nitrates, niacin, phenylephrine, LSD, MDMA
30
In regards to drug elimination, _______ are trapped in urine and cleared quickly. ____ \_\_\_\_\_\_ can be reabsorbed
Ionized species are trapped in urine and cleared quickly. Neutral forms can be reabsorbed
31
Examples of Weak acids (4)
Weak acids
Asprin, Methotrexate, Phenobarbital, Warfarin
WAMP - you're hit with a Weak Acid
W-arfarin
A-sprin
M-ethotrexate
P-henobarbital
32
If TCAs are weak bases, why do we treat TCA overdose with sodium bicarbonate (instead of maybe ammonium chloride to acidify the urine and inc elimination of the weak base)
TCA toxicity is generally treated with sodium bicarbonate to overcome the sodium channelblocking activity of TCAs, but not for accelerating drug elimination.
33
Examples of Weak Bases
TCAs, Amphetamines
Weak Bases = MAT DACes
| (Allopurinol, Diazepam, Cocaine, Methyldopa)
34
What drugs would be cleared by acidifying the urine?
Acidifying urine --\> inc ionization of **weak bases** to inc renal elimination.
35
What do we give to alkalinize urine?
NaHCO3, potassium citrate
36
What do we give to acidify urine?
Ammonium chloride, Vitamin C, Cranberry juice
37
Drugs with zero order kinetics?
Rate of elimination is constant regardless of Cp (ie, constant amount of drug eliminated per unit time). Cp decreases linearly with time.
_high dose or toxic concentration_
* Phenytoin
* Ethanol
* aspirin
_Toxic dose_
Salicylates, Cisplatin, Flouxetin, Omeprazole
38
What happens in phase I drug metabolism?
**R**eduction, **O**xidation, **H**ydrolysis with cytochrome P-450 usually yield slightly polar, water-soluble metabolites (often still active).
R-OH = Phase I
39
What happens in phase II drug metabolism?
Conjugation (Methylation, Glucuronidation, Acetylation, Sulfation) usually yields very polar, inactive metabolites (renally excreted).
40
Which phase of drug metabolism do the elderly lose first?
Phase I
41
Patients who are slow acetylators have ___ side effects from certain drugs because of \_\_\_\_\_rate of metabolism (eg, isoniazid).
Patients who are slow acetylators have **inc** side effects from certain drugs because of **dec** rate of metabolism (eg, isoniazid).
42
What value of a drug curve represents efficacy?
y-intercept = Vmax
the higher the Y intercept, the higher the Vmax, the higher the efficacy
43
How is efficacy related to potency?
Unrelated to potency (ie, efficacious drugs can have high or low potency)
44
Safer drugs have higher _____ values.
Safer drugs have higher TI values.
45
What are drugs with lower TI values that req monitoring?
* *W**arfarin, **The**ophylline, **D**igoxin, **A**ntiepileptic drugs, **L**ithium;
* *W**arning! **The**se **D**rugs **A**re **L**ethal!).
46
47
Adrenal medulla is directly innervated by __________ \_\_\_\_\_\_\_\_\_\_ \_\_\_\_\_\_\_\_.
Adrenal medulla is directly innervated by preganglionic sympathetic fibers.
48
Sweat glands are part of the\_\_\_\_\_\_ _____ but are innervated by _________ \_\_\_\_\_\_\_
Sweat glands are part of the sympathetic pathway but are innervated by cholinergic fibers
49
What is the channel assoc with nicotinic Ach receptors?
ligand gated Na/K channels
50
Subtypes of nicotinic Ach receptors
Two subtypes: NN (found in autonomic ganglia, adrenal medulla) and NM (found in neuromuscular junction of skeletal muscle).
51
Muscarinic Ach Receptors work through which receptors?
Muscarinic ACh receptors are G-protein–coupled receptors that usually act through 2nd messengers
52
Subtypes of Muscarinic Ach-R
5 subtypes: M1–5 found in heart, smooth muscle, brain, exocrine glands, and on sweat glands (cholinergic sympathetic).
53
G protein class of α1 & α2 rec'r?
α1 - Gq
α2 - Gi
54
Major fxn of α1-R?
Inc vascular smooth muscle contraction
Inc pupillary dilator muscle contraction (mydriasis)
Inc intestinal and bladder sphincter muscle contraction
55
Major fxn of α2-R?
dec sympathetic (adrenergic) outflow
dec insulin release,
dec lipolysis,
dec aqueous humor production
Inc platelet aggregation,
56
G protein class of β1, β2, β3 - R?
All are Gs
57
What g proteins are affiliated with M1-3 receptors?
M1R = Gq
M2R = Gi
M3R = Gq
58
Fxn of M1R
Mediates higher cognitive functions, stimulates enteric nervous system
59
Fxn of M2R
dec heart rate and contractility of atria
60
M3R fxn?
* Inc exocrine gland secretions (eg, lacrimal, sweat, salivary, gastric acid)
* Inc gut peristalsis,
* Inc bladder contraction,
* **bronchoconstriction,**
* Inc pupillary sphincter muscle contraction (miosis), ciliary muscle contraction (accommodation),
* **Inc insulin release,**
* **endothelium-mediated vasodilation**
61
The two dopamine receptors have what g proteins as 2nd messangers?
D1R - Gs
D2R - Gi
62
Fxn of D1R & D2R
D1R - **Relaxes renal vascular smooth muscle**, activates direct pathway of striatum
D2R - Modulates transmitter release, especially in brain, inhibits indirect pathway of striatum
63
What g proteins are associated with histamine receptors?
H1R - Gq
H2R - Gs
64
Fxn of H1R & H2R
H1R
inc nasal and bronchial mucus production, vascular permeability, bronchoconstriction, pruritus, pain
H2R
inc gastric acid secretion
one - lung, two - stomach
65
Vasopressin receptors - what g protein?
V1R - Gq
V2R - Gs
66
Fxn of V1R & V2R?
V1R - Inc vascular smooth muscle contraction
V**2**R - inc H2O permeability and reabsorption via upregulating aquaporin-**2** in collecting **two**bules (tubules) of kidney, **inc release of vWF**
67
Release of norepinephrine from a sympathetic nerve ending is modulated by ___ itself, acting on ______ \_\_\_\_\_\_\_\_\_\_\_
Release of norepinephrine from a sympathetic nerve ending is modulated by NE itself, acting on presynaptic α2-autoreceptors --\> negative feedback.
68
69
70
With cholinomimetic drugs - what should one be on the look out for?
Watch for exacerbation of COPD, asthma, and peptic ulcers in susceptible patients.
71
Rx used for urinary retention - MoA?
Bethanechol - Activates bladder smooth muscle; resistant to AChE. No nicotinic activity
72
Cholinomimetic rx used to relieve intaocular pressure in open angle glaucoma?
Carbachol - **Carb**on copy of **a**cetyl**chol**ine (but resistant to AChE).
Carba**chol** for glau**Coma**
73
Used to test for asthma? MoA?
Methacholine - asthma challenge test - (+) muscarinic receptor in airway when inhaled
74
Cholinomimetic rx that is used to treat glaucoma and the dry mouth of Sjogren?
Pilocarpine
75
MoA of Pilocarpine?
Contracts ciliary muscle of eye (open-angle glaucoma), pupillary sphincter (closed-angle glaucoma);
resistant to AChE, can cross bloodbrain barrier (tertiary amine).
“You cry, drool, and sweat on your ‘pilow.’ ”
76
Rx 1st line for Alzheimer disease
Donepezil, rivastigmine, galantamine
77
Rx that was used to Dx MG? What is used now?
Edrophonium;
replaced by anti-AchR Ab
78
Use of Neostigmine?
* Postoperative and neurogenic ileus and urinary retention,
* myasthenia gravis
* reversal of neuromuscular junction blockade (postoperative).
NEO - NEuromusc NEurogenic retention post Op
79
Tx for anticholinergic toxicity?
Physostigmine
"Phy-xes" (Fixes) anticholingeric tox
Physo-therapy for anticholinergic tox
80
What drugs are used to control the side effects of Pyridostigmine?
Used with glycopyrrolate, hyoscyamine, or propantheline to control pyridostigmine side effects.
Use GHP drugs to put Pyrido to sleep (Like GHB)
81
Pyridostigmine used for what disease? and why?
MG; long acting, does not penetrate CNS
82
Affects of organophosphates
How to reverse organophosphate poisoning?
Diarrhea
Urination,
Miosis,
Bronchospasm,
Bradycardia,
Emesis,
Lacrimation,
Sweating,
Salivation.
DUMBBELSS
Rx/ Atropine
83
What are the nicotinic effects of organophosphate poisoning?
Neuromuscular blockade;
like succinyl choline
84
How to reverse the nicotinic effects of organophosphates?
Pralidoxime; regenerates AchE if given early
How to rev. nicotinic effects of organophosphates.
PraLID O - Put a LID on nicOtinic effects.
85
CNS effects of organophosphate poisoning?
respiratory depression,
lethargy,
seizures, coma
86
Atropine, homatropine, tropicamide works on what body part? used for what?
Atropine, homatropine, tropicamide:
to produce mydriasis and cycloplegia
87
Benztropine; trihexyphenidyl has what site of action and application?
**Benz**tropine; **tri**hexyphenidyl
used in CNS, for Parkinsons and acute dystonia
Try to Park my Benz
88
Glycopyrrolate has what use in the body?
Glycopyrrolate
Parenteral: preoperative use to reduce airway secretions.
Oral: drooling, peptic ulcer.
89
Hyoscyamine
Dicyclomine
Hyoscyamine Dicyclomine:
HolD the spasms
GI - antispasmodics for IBS
90
Ipratropium and tiotropium
respiratory;
COPD, asthma (“I pray I can breathe soon!”)
91
What muscarinic antagonist is used against bladder spasms and urge urinary incontinence?
Bladder spasms and urinary incontinence
Solifenacin
Tolterodine
Oxybutynin
STOP urinary incontinence
Ephedrine (pseudophedrine)
92
used for motion sickness
Scopolamine
93
Atropine effects on?
94
Atropine blocks ______ effects of anticholinesterases, but not the _____ effects.
Atropine blocks _muscarinic_ effects (DUMBBeLSS) of anticholinesterases, but not the _nicotinic_ effects.
95
SE of Atropine
inc body temperature (due to dec sweating); Inc HR; dry mouth; dry, flushed skin; cycloplegia; constipation; disorientation
Hot as a hare
Dry as a bone
Red as a beet
Blind as a bat
Mad as a hatter
Full as a flask
96
What can atropine use lead to in the elderly, in men, and infants?
Atropine use causes:
Can cause acute angle-closure glaucoma in elderly (due to mydriasis), urinary retention in men with prostatic hyperplasia, and hyperthermia in infants.
97
Albuterol,salmeterol, and terbutaline works on which receptors? used for?
β2 \> β1
Albuterol for Acute asthma/COPD.
Salmeterol for Serial (long-term) asthma/COPD.
Terbutaline for acute bronchospasm in asthma and tocolysis.
98
Dobutamine - rec'r and use?
```
β1 \> β2, α
Heart failure (HF), cardiogenic shock (inotropic \> chronotropic), cardiac stress testing.
```
99
Dopamine - which rec'r and use?
D1 = D2 \> β \> α
Unstable bradycardia, HF, shock;
inotropic and chronotropic effects at lower doses due to β effects;
vasoconstriction at high doses due to α effects
100
Difference between Epi/NE and receptors they use?
Epi = β \> α
NE = α1 \> α2 \> β
101
Epi and NE used for?
Epi - Anaphylaxis, asthma, open-angle glaucoma; α effects predominate at high doses. Significantly stronger effect at β2-receptor than norepinephrine.
NE - Hypotension, septic shock
102
Fenoldopam - which rec'r and use?
D1 R
Postoperative hypertension, hypertensive crisis. Vasodilator (coronary, peripheral, renal, and splanchnic).
Promotes natriuresis.
Can cause hypotension and tachycardia.
**Feno**ldopam - **FEN**d **O**ff serious HTN
103
Isoproterenol - affect which rec'r ? use?
β1 = β2
Electrophysiologic evaluation of tachyarrhythmias. Can worsen ischemia.
Has negligible α effect.
104
rec'r used by Midodrine, what use?
α1
Autonomic insufficiency and postural hypotension. May exacerbate supine hypertension
105
Mirabegron - rec'r and use?
Mirabegron
β3
urinary incontinence, overactive bladder
Beta 3 = inc lipolysis, thermogenesis, bladder relaxation
106
Phenylephrine - rec'r and use?
α1 \> α2
Hypotension (vasoconstrictor), ocular procedures (mydriatic), rhinitis (decongestant), ischemic priapism.
vascular smooth muscle contraction, pupillary dilator muscle contraction (mydriasis), intestinal and bladder sphincter muscle contraction
107
List 3 indirect sympathomimetics
Amphetamine
Cocaine
Ephedrine
(TCAs)
108
List the mechanisms of Amphetamine, Cocain, Ephedrine
Amphetamine - Indirect general agonist, reuptake inhibitor, also releases stored catecholamines
Cocaine - Indirect general agonist, reuptake inhibitor Ephedrine - Indirect general agonist, releases stored catecholamines
109
Why is it dangerous to give BB to a cocaine user?
Caution when giving β-blockers if cocaine intoxication is suspected (can lead to unopposed α1 activation --\> extreme hypertension, coronary vasospasm).
110
Use of Ephedrine
Nasal decongestion (pseudoephedrine), urinary incontinence, hypotension
111
used for hypertension in pregnancy
α-methyldopa
112
SE of α-methyldopa
**D**irect Coombs ⊕ hemolysis, **d**rug-induced lupus
α-methyl**d**opa
113
Other drugs that cause drug (+)'d lupus
Drugs that cause COOMBS (+) hemolysis
Lupus
Methyldopa, Minocycline, Hydralazine,
Isoniazid, Phenytoin, Sulfa drugs, Etanercept,
Procainamide
Lupus Makes My HIPS Extremely Painful
M SHIPPE
Coombs: Penicillin, methylDopa, Cephalosporins
114
sympatholytic that relieves spasticity
Tizanidine
Spastic Tizan
115
Clonidine and Guanfacine applications
Clonidine and Guanfacine - alpha 2 agonists
( dec sympathetic (adrenergic) outflow, dec insulin release, dec lipolysis, dec aqueous humor production, INC plat aggregation)
Hypertensive urgency (limited situations), ADHD, Tourette syndrome, symptom control in opioid withdrawa
116
if one abruptly stops taking clonidine/guanfacine, what is the side effect
rebound hypertension
117
side effects of α-methyldopa
Direct Coombs ⊕ hemolysis, drug-induced lupus
118
Use of Tizanidine & SE.
Relief of spasticity
Hypotension, weakness, xerostomia
119
Diff b/w Phenoxybenzamine & Phentolamine
Phenoxybenzamine - irreversible α-blocker
Phentolamine - reversible α-blocker
120
Use of Phenoxybenzamine
Pheochromocytoma (used preoperatively) to prevent catecholamine (hypertensive) crisis
121
α2 selective (-)'r and use
Mirtazapine, use for depression
MirtAZapine = α2
(DEC sympathetic (adrenergic) outflow, insulin release, lipolysis, , aqueous humor production INC platelet aggregation)
122
Examples of partial agonists?
* **Danazol - partial agonist at androgen receptor**
* acebutalol - B1 sel partial agonist
* pindalol - BB, nonselective
* **Tamoxifen - partial agonist in endometrium (SERM)**
* **Buprenorphine - partial agonist at opiod receptor**
* **Aripiprazole - D2 partial agonist**
* Varenicline - nACh-R partial agonist
* Vilazodone - 5HT1A-R partial agonist
* Buspirone - 5HT1A-R partial agonist
* Butorphanol - mu partial agonist (mixed opiod receptor)
* Pentazocine - mu antagonist/partial agonist (mixed opiod)
123
Which beta blockers dec mortality in heart failure?
Bisoprolol, Carvedilol, Metoprolol (β-blockers Curb Mortality
124
In HTN how do BB help?
dec cardiac output, dec renin secretion (due to β1 receptor blockade on JG cells)
125
BB used in hyperthyroidism, actions?
Propranolol
Symptom control (dec heart rate, dec tremor), thyroid storm
126
How do BB help in hypertrophic cardiomyopathy
dec heart rate --\> inc filling time, relieving obstruction
127
How do BB help in MI?
dec o2 demand
dec mortality
128
Which BB used for SVT? how do they help?
metoprolol
esmolol
dec AV conduction velocity (class II antiarrhythmic)
MESsVT - **M**etoprolol & **Es**molol for **SVT**
129
BB used in variceal bleeding? MoA?
Nadolol, propranolol, carvedilol
dec hepatic venous pressure gradient and portal hypertension (prophylactic use)
Portal VariCeal hypertensioN
P - propranolol
C- Carvedilol
N- nadolol
130
Adverse effects of BB
* Erectile dysfunction
* cardiovascular (bradycardia, AV block, HF),
* CNS (seizures, sleep alterations)
* dyslipidemia (metoprolol)
* asthma/COPD exacerbations
131
Why must one be wary of using BB in cocaine assoc chest pain?
Use of β-blockers for acute cocaine-associated chest pain remains controversial due to unsubstantiated concern for unopposed α-adrenergic stimulation.
132
Ex of B1R (-)'rs?
β1-selective antagonists (β1 \> β2)—acebutolol (partial agonist), atenolol, betaxolol, bisoprolol, esmolol, metoprolol
133
Nonselective α- and β-antagonists?
carvedilol
labetalol
134
Unique features of Nebivolol?
Nebivolol combines cardiac-selective β1-adrenergic blockade with stimulation of β3-receptors (activate nitric oxide synthase in the vasculature and dec SVR)
**N**ebiv**o**lol inc **NO**
135
What type of foods can lead to histamine poisoning?
Spoiled dark-meat fish such as tuna, mahimahi, mackerel, and bonito.
136
Action of histamine in scombroid poisoning, and sx?
Bacterial histidine decarboxylase converts histidine to histamine. Frequently misdiagnosed as fish allergy.
Mimics anaphylaxis: acute burning sensation of mouth, flushing of face, erythema, urticaria, itching. May progress to bronchospasm, angioedema, hypotension.
137
Tx of Histamine poisoning?
Antihistamines. Albuterol and epinephrine if needed.
138
Tetrodotoxin - found in what food? MoA?
Pufferfish. Highly potent toxin; binds fast voltagegated Na+ channels in cardiac/nerve tissue, preventing depolarization
139
Sx of TTX poisoning?
Nausea, diarrhea, paresthesias, weakness, dizziness, loss of reflexes.
140
Ciguatoxin found in what food?
Reef fish such as barracuda, snapper, and moray eel.
141
MoA and Sx of ciguatoxin?
Opens Na+ channels, causing depolarization.
Nausea, vomiting, diarrhea; **perioral numbness; reversal of hot and cold sensations**; bradycardia, heart block, hypotension.
142
What is Beers criteria ?
Widely used criteria developed to reduce potentially inappropriate prescribing and harmful polypharmacy in the geriatric population. Includes \> 50 medications that should be avoided in elderly patients due to **dec efficacy and/or inc risk of adverse events**
143
Ex of Rx that meet Beers criteria?
* α-blockers (inc risk of hypotension)
* Anticholinergics, antidepressants, antihistamines, opioids (inc risk of delirium, sedation, falls, constipation, urinary retention)
* Benzodiazepines (inc risk of delirium, sedation, falls)
* NSAIDs (inc risk of GI bleeding, especially with concomitant anticoagulation)
* PPIs (inc risk of C difficile infection)
144
A man presents with kidney issues and pain - what Rx should one be careful giving him? and why?
Morphine - Morphine 6 glucoronide is an active metabolite of morphine and more active than morphine itself. Can be toxic in pt. with kidney issues, since they can't eliminate it as well
145
A pt has a clotting issue, but is a poor metabolizer. What anti-clotting Rx should we not give him?
Not Warfarin - Poor metabolizers will bleed.
146
A pt is on Warfarin but acquires a bacterial infection - which antibiotics would cause bleeding in this patient?
Ciprofloxacin, Macrolides (except azithromycin), Sulfonamides.
147
5 drugs that cause pulmonary fibrosis?
Bleomycin (w/in weeks -mos), Amiodarone, Busulfan (takes years), Methotrexate, Nitrofurantoin
Pulmonary fibrosis is BBAd, MaN
148
Why does Crohn's lead to malabsorption?
Crohn's has cobblestone mucosa - the thicker membrane is due to fibrosis, decreasing the absorption in SI
149
What form of a drug is needed to get into the CNS?
lipid soluble, Non-ionized, small
150
what form of drug is affected by pK and pH?
Ionized, water soluble
151
Why is Heparin the anticoagulant of choice in pregnancy?
water soluble, won't cross blood placental barrier
152
Drug of Choice in hypothyroidism in pregnancy?
PTU, 90% protein bound, wont cross blood placental barrier
153
Which Rx would decrease Digoxin's Vd (volume of distribution) (6)
Any Rx that displaces digoxin from its tissue binding site (more tissue bound = greater Vd) - Amiodarone, verapamil, itraconazole, erythromycin, clarithromycin, quinidine.
154
Disruption of which metabolic pathway will lead to poor drug metabolization by cytochromes?
Pentose phosphate pathway - Cytochrome p450s require NADPH to function
155
How many half lives does it take to get to 90% of steady state?
3.3
156
What drug reverses the action of Heparin? (Chemical antagonism)
Protamine sulfate
157
Which drugs bind to an inhibitory Cl- ion channel in the CNS?
GABAa Receptor - Benzos, Barbiturates,
158
Which receptors will result in DEC in cAMP? (6)
Gi coupled -
*M***2**R, ***A***lpha**2**-R, *D***2**R, - People who are 2 MAD (-) themselves
Opiate, GABAb, 5-HT1
159
Which receptors activate PLC?
Gq coupled -
a1-R, M1-R, M3-R, H1, V1, - **HAVE 1 M&M**
5-HT2
160
Example of tyrosine kinase receptor blocker? Used for what diseases?
Imatinib - CML, GI stromal tumors Erlotinib - non small cell lung carcinoma
161
Single most effective drug for malaria? SE?
Artesunate \> Quinidine/Doxycyclin - clears parasitemia faster SE// long QT
162
\_\_\_\_\_\_ is directly proportional to the enzyme concentration
Vmax is directly proportional to the enzyme concentration
163
Max concentration of a drug is proportional to ?
Dose administered
164
Which antibiotic is contraindicated in neonate because it could lead to kernicterus? why?
Sulfonamides, as they displace bilirubin from albumin binding sites.
