Pharmacology Flashcards
1
Q
Statins
A
- Treats hypercholesterolemia by inhibiting HMG-CoA reductase (inhibition of cholesterol synthesis)
- Leads to increased LDL receptor expression to increase LDL uptake
2
Q
Oseltamvir
A
- Treats and prevents BOTH influenza A and B
- Impairs virion release by inhibiting NeurAminidase
- Prevents viral penetration of mucous secretions in respiratory epithelium
3
Q
PTU
A
-Inhibits both organification of iodine (via thyroid peroxidase inhibition) AND peripheral conversion of T4 to T3
(Methimazole: only does inhibition of iodine organification)
4
Q
MTX
A
Structurally similar to folate → irreversibly inhibits DHFR –> polyglutamated form (cannot move out of cell)
5
Q
Ergonovine
A
Ergot alkaloid that can provoke coronary vasospasm
6
Q
Bepridil
A
Ca2+ channel blocker used 2nd line as angina therapy, not used as an anti-hyprtensive
7
Q
Ceftriaxone resistance:
A
by either beta-lactamases or altered PBP structure
8
Q
Niacin’s Mechanism and Side Effects
A
- Inhibits hepatic VLDL production and triglycerides
- increases HDL
- Acute gout flare is a possible side effect
- Hyperuricemia, hyperglycemia, and flushing
- Flushing can be reduced with Aspirin pretreatment
9
Q
Nitrate Tolerance
A
Nitrates develop tolerance quickly so much have a nitrate free period every day
10
Q
Mu Receptors
A
- opioids bind
- increase potassium efflux → hyperpolarization
11
Q
Tx of Gouty Arthritis
A
NSAID, colchicine, and then glucocorticoids
- Uricosuric agents or Xanthine Oxidase inhibitors contraindicated in acute attacks (can worsen it); but they are good for prophylaxis
12
Q
Antiarrhythmics Na+ Channel Binding Strength
A
1C > 1A > 1B
- Use dependence more prominent in 1C ( higher rates of depolarization → increased channel blockade because less time in resting state)
13
Q
Reverse Use Dependence
A
Class III: K+ Channel Blockers
14
Q
Minimal alveolar concentration (MAC):
A
% of anesthetic in inspired gas mixture that renders half of patients unresponsive to painful stimuli
- Lower the MAC, the higher the potency
- If anesthetics have a high blood/gas coefficient (meaning they dissolve more in blood), they will have a slower onset of action
15
Q
ABPA
A
Asthma with aspergillus; high eosinophilia
16
Q
Physostigmine
A
Cholinesterase inhibitor (Ach builds up); similar to edrophonium - Both peripherally and centrally
17
Q
Pilocarpine
A
Cholinergic Agonist
18
Q
Phentolamine and Phenoxybenzamine
A
a-adrenergic antagonist
- Phentolamine has a half life of 20 min (irreversible)
- Phenoxybenzamine has a half life of 24 hours and is often used to treat pheochromocytoma (reversible)
19
Q
Phenylephrine
A
a-adrenergic agonist
20
Q
Amiodarone
A
Delayed onset interstitial pneumonitis + a lot of other side effects
21
Q
Mifepristone
A
Inhibits progesterone receptors (induce abortion)
- Used with Misoprostol: PGE1 analog
22
Q
Aspirin
A
Inhibition of COX pathways → promotes formation of leukotrienes that cause bronchoconstriction
23
Q
Alpha 1, 2, beta 1 ,2 m 1-3. D1-2, H1-2, Vasopressin 1-2
A
QISS QIQ SIQ SQS
- Q: phospholipase C → DAG, IP3
- S: stimulate Adenylate cyclase → cAMP increase
- I: inhibit Adenylate cyclase → cAMP decrease
24
Q
Red Man Syndrome
A
- Rapid infusion of vanco → red man syndrome due to widespread release of histamine (NOT IgE mediated allergic reaction)
- Can be prevented with a slower rate of infusion
25
Michaelis Menten
Y intercept - Vmax (up means decrease)
- Vmax is directly proportional to concentration
X intercept – Km (closer to Y line → Km increases → lesser affinity)
26
COX1
- In platelets prevents thromboxane formation (preventing platelet aggregation)
- Also does gastric protection
(Problem with NSAIDs)
- Selective COX 2 inhibitors (celecoxib) are good for pain (no effect on gastric mucosa)
27
Tx for MRSA
Ceftaroline (5)
- Vancomycin
- Daptomycin
- Linezolid
- Tigecycline
28
Pseudomonas Tx:
- Ceftazidime (3) and Cefepime (4)
| - Ticarcillin or piperacillin (w/ clavulanate, tazobactam or sulbactam)
29
Cephalosporin Generations:
1: faz, phal
2: fox, fac, fur
3: tri, trax, tax
4: cefepime
5: ceftaroline
30
B-lactam that can be used in PCN Allergies
Aztreonam
31
Gram (-) Rod Tx:
aztreonam, cephalosporins (3), aminoglycosides
32
Gm (+):
vanco
33
Always give carbapenems:
cilastatin (it inhibits renal tubular secretion of the antibiotic)
eg. similar to giving penicillin w/ probenecid
34
Aminoglycosides
30s, misread mRNA (inhibiting initiation complex formation)
| eg. gentamicin, amikacin, tobramicin
35
Tetracyclines
30s, block tRNA binding site
- For intracellular (rickettsia, mycoplasma, borrelia, chlamydia) (eg. Doxycycline)
eg. tetracyline, doxycycline, minocycline
- binds inorganic compounds (in bone and teeth) causing teeth discoloration and retarded bone formation
36
Linezolid
50s, blocks 70s formation
37
Chloramphenicol
50s, blocks peptidyl transferase
38
Macrolides
50S, blocks translocation (binds the 23S part of 50s)
Atypical pneumonia, STDs, Gm + cocci
eg. clarithromycin, erythromycin, azithromycin
39
Clindamycin
50S, blocks translocation (binds the 23S part of 50S)
- Anaerobes, GAS
- Causes C. Diff
40
Fluoroquinolines
(floxacins) inhibit DNA gyrase
| - Atypical pneumonias, Gm – rods
41
Metronidazole
Makes free radicals to break DNA
| - D. diff, gardnerella, giardia, anaerobes
42
Isoniazid
Decreased mycolic acid synthesis (must be activated with catalase peroxidase)
- 2 Mechanism of resistance:
decreased expression of catalase peroxidase or modification of protein target binding site
- may cause pyridoxine deficiency; acetylated for excretion (slow acetylators have increased risk of toxicity)
- Also is directly hepatotoxic in 10-20%
43
Rifampin
Inhibits DNA dep RNA pol
| - Prophylaxis for meningococcal and Hib
44
Ethambutol
Inhibits mycobacterial cell wall synthesis by blocking arabinosyl transferase (inhibits carbohydrate polymerization
- central scotomas
45
Amphotericin B and Nystatin
Binds ergosterol and makes pores
| Nystatin: topical because too toxic
46
Griseofulvin
Binds microtubules and inhibits mitosis (antifungal)
| Also induces P450
47
Terbinafine
Inhibits fungal squalene epoxidase
48
Caspofungin
Inhibits cell wall synthesis (by inhibits b-glucan)
49
Inhaled gas anesthetics
- Poorly Soluble gas: saturates quickly, so partial pressure starts to rise, rapid equilibration with
- Highly soluble gas: saturates more slowly so need more to saturate, slower rise in partial pressure so lower onset and equilibration
50
Lipophilic Drugs
- Highly lipophilic drugs are preferentially metabolized by liver (poorly eliminated by kidney)
51
Milrinone
PDE3 inhibitor → increases cardiac contractility
52
Opioids: Tolerance Does Not Develop for _______
Miosis and constipation
53
Nitroglycerin has greatest effect on:
Large veins
54
Statin Metabolism
Metabolized by P450 (except pravastatin), inhibitors will increase concentration → more rhabdomyolysis → acute renal failure
55
CYP450 Inhibitors
```
Cimetidine
Ciprofloxacin
Erythromycin
Azoles
Grapefruit juice
Isoniazid
Ritonavir
```
56
Permissive
Something with no effect, will increase the effect of something else
57
Additive
When combined effect of drugs together is equal to the sum of their individual effects
58
Synergistic
Combined effect exceed the effect of the sum of both effects
59
Bile Acid Binding Resins (eg. Cholestyramine) Side Effect
- Cholesterol Gallstones (prevent absorption, so liver makes more cholesterol)
- Mild increase in triglycerides
60
Tx to Decrease Triglycerides
Fibrates (1st line) and Niacin
61
Clonidine
a2 agonist
| - decreases peripheral vascular resistance
62
MTX vs 5FU
- MTX prevents reduction of TH4 while 5FU binds TH4 and thymidylate synthase in a stable intermediate form which decreases the amount of thymidylate synthase available
- 5FU cannot be overcome with addition of folinic acid or leucovorin
63
Beta Blockers Effect on AV Conduction
Slow AV conduction which prolongs the PR interval
64
Niacin Induced Flushing Due to:
Prostaglandins
65
Vancomycin Induced Flushing Due to:
Histamine (can be limited with slow infusion and anti-histamine treatmeant ahead of time)
66
Weight Loss Drugs
- dexfenfuramine, phenteramine, fenfluramine
| - can cause cor pulmonale
67
Tx for Methanol or Antifreeze (ethylene glycol) Poisoning
Fomepizole (alcohol dehydrogenase inhibitor)
68
Tx for Arsenic, Lead, Mercury & Gold Poisoning
Dimercaprol
| - EDTA can also be used for lead
69
Demeclocycline
- Tetracycline antibiotic that can be used to treat SIADH
70
Conivaptan or Tolvaptan
ADH Receptor Antagonists used to treat SIADH
71
Raltegravir
Integrase inhibitor that prevents HIV from integrating into chromosome of Host so host cell machinery cannot be used to make HIV mRNA
72
Entacapone and Tolcapone
- COMT inhibitor that increases bioavailability of levodopa by decreasing peripheral methylation
- Tolcapone inhibits BOTH peripheral and central methylation
73
SGTP2 inhibitors (eg. Canaglifozin)
- Lose glucose in urine due to osmotic diuresis
- Need to check renal status before using
- Can cause yeast infection
74
DPP4 inhibitors
prevent degradation of GLP to prolong its action in increasing insulin
(–gliptins)
75
GLP1 Analogs
Exenatide or Liraglutide
76
Ketoconazole
Inhibits testosterone synthesis pathways
77
Adrenergic, Muscarinic, Dopaminergic, Histamine, Vasopressin
QISS QIQ SIQ SQS
Q: GPCR
S: increase cAMP
I: decrease cAMP
78
CYP450 Inducers
Phenytoin, Phenobarbital, Rifampin, Carbamazepine, Griseofulvin
79
DRESS syndrome
Adverse drug reaction w/ eosinophilia
80
Low Volume of Distribution If:
Trapped in plasma
| - Due to high MW, high plasma protein binding, hydrophilicity and high charge
81
High Volume of Distribution If:
Lipophilic, unbound, low charge, low MW can cross membranes more easily and access intracellular compartment → very large Vd
82
HAART
NNRTI: DEN (efavirenz)
Protease inhibitors: -navir
Integrase inhibitors: -tegra-
NRTI: everything else
83
Inhibitors of dihydrofolate reductase
Trimethoprim, methotrexate, and pyrimethamine
84
Pavilizumab
For RSV prevention: Ab to F (fusion) protein
85
Zidovudine
NRTI used to treat HIV: causes bone marrow suppression especially with gancyclovir
- Competitively binds reverse transcriptase and is incorporated as thymidine analog and since it does not have a 3OH group, cannot make 3-5' phosphodiester bond
86
Protease inhibitors: side effects
hyperglycemia, lipodystrophy, and p450 inhibition
87
NNRTI
Do not require phosphorylation
| - MC ones include: Nevirapine, Efavirenz, and Delaviridine
88
TNF-a Inhibitors
may reactivate latent TB by decreasing macrophage function (maintain granulomas)
- Cord Factor (virulence) in Mycobacteria inhibits macrophage activation and TNFa release
89
TNF-a is the main mediator of:
- Paraneoplastic cachexia (wasting syndrome)
| - Sepsis (also IL-6 and IL-1 are part of the response)
90
Alemtuzumab
CD52 inhibitor used for CLL
91
Cetuximab
EGFR antibody for colorectal and head/neck cancers
92
Natalizumab
Ab to a4-integrin for MS and Crohns
| - Risk of PML from JC virus
93
Azathioprine/6-MP degraded by:
xanthine oxidase (which is inhibited by allopurinol) and TPMT in liver
94
ACE Inhibitors
Angioedema side effect (c1 inhibitor deficiency)
- ACE made in lung endothelium
- Don’t use in patients with bilateral renal artery stenosis → ARF (acute renal failure) because they are dependent on ACE for renal blood flow (can no longer constrict efferent arteriole to maintain GFR)
95
IFN's
IFNa- hepC
IFNb- MS
IFNy- for CGD
96
Ribavirin
HepC and RSV
| - Inhibits RNA poly and IMP dehydrogenase → interferes with duplication of viral genome
97
Isoniazid
Must be activated by catalase peroxidase enzyme
- Inhibits mycolic acid synthesis (TB no longer is acid fast)
- Metabolized by acetylation → excreted in urine
98
Pyrazinamide
works best in an acidic environment to kill intracellular organisms like TB
99
Ondansetron and Metoclopramide work on:
floor of 4th ventricle
Ondensetron is a 5HT3 antagonist
Metoclopramide is a dopamine receptor antagonist (don't use in parkinson's patients)
100
Thiopental
Short acting anesthetic barbiturate
- After equilibrating in brain (takes about 1 min) it redistributes quickly to skeletal muscle and fat (resulting in rapid recovery from anesthesia)
101
Acetazolamide
Carbonic anhydrase inhibitor
- Can be used to treat narrow-angle glaucoma
- Works in proximal tubule of nephron
- Can cause metabolic acidosis by blocking NaHCO3 reabsorption
102
Succinylcholine (Neuromuscular Blockade)
May cause hyperkalemia (peak T waves)
- Burn pts more at risk because of leaking/damaged cells
- Strong Ach receptor agonist --> sustained depolarization (prevents muscle contraction)
- Antidote only for Phase II: ACHE inhibitors (eg. neostigmine)
- May cause malignant hyperthermia
103
Beta Blockers w/ Diabetics and Asthma/COPD
Diabetics w/ HTN → it can mask hypoglycemia
- Use an ACE inhibitor instead (prevents diabetic nephropathy)
- Can also exacerbate asthma and COPD
104
Essential Tremor Tx
Non-selective Beta Blocker or Primidone
105
Benadryl and Dramamine
- Diphenhydramine = Benadryl
| - Dimenhydrinate = Dramamine
106
2nd Generation (histamine) H1-receptor blockers
Less side effects because does not cross BBB
| - Loratidine, desloratidine, fexofenadine, cetirizine
107
Tx for UTI in Children
amoxicillin (w/ or w/out clavulanate), cefixime, ceftriaxone, cephalexin, nitrofurantoin, or sulfamethoxazole/trimethoprim
108
_________ are less effective when taken with Antacids
Fluoroquinolones (DNA gyrase inhibitors)
109
PCN allergy cross-allergenicity w/:
Cephalosporins
110
Chloramphenicol: Side effect
Can cause pancytopenia
111
Daptomycin
- Aw/ increased CPK and incidence of myopathy
- For gram + only
- Makes pores
112
Half-Life
t1/2 = (.7*Vd)/Cl
113
Treat Carcinoid Syndrome w/
Octreotide
114
Drug Efficacy
maximum effect of a drug (regardless of dose)
115
Competitive Antagonist
```
Changes ED50 (effective dose/potency): shift right
- Need a higher dose to overcome antagonist
```
116
Noncompetitive OR Irreversible competitive antagonist
```
Changes Emax (max effect/efficacy): shift down
- Increasing the dose will not help
```
117
Partial Agonist
Decreases max effect; variable potency
118
Tacrolimus
prevents Transcription of IL2; FKBP; Calcineurin inhibitor
| - causes hyperglycemia
119
Sirolimus
prevents Signal transduction of IL2; MTOR
120
Cyclosporine
prevents Transcription of IL2: Calcineurin inhibitor
| - nephrotoxic
121
Cimetidine: P450 effect
can decrease P450 metabolism of warfarin → easy bruising and bleeding
122
Anticholinergic Side Effects
hot as a hare, dry as a bone, blind as a bat, red as a beet, mad as a hatter
123
Rasburicase
effective in preventing and treating hyperuricemia and its renal manifestations from tumor lysis syndrome (it is similar to allopurinol)
124
Aminoglycosides must be administered _________
Parenterally
125
Anesthetics that block Na Channels
- Amide types have 2 I’s in the name
- Ester types have only one i
- Important to remember if a patient has an allergy to one type, can use the other type because there is no cross reaction
- Inhaled anesthetics (esp halothane) → hepatotoxicity (necrosis/shunken)
126
Foscarnet
- pyrophosphate analog that does NOT require activation
- Inhibits RNA pol (in herpesvirus) and reverse transcriptase (in HIV)
- for CMV
- Side effects: Hypocalcemia, hypomagnesia
127
Cidofovir
- does not require phosphorylation
| - for CMV
128
Amphotericin B: can cause arrhythmias due to:
hypokalemia and hypomagnesia
129
Metformin contraindicated in:
renal failure
130
Heparin for DVT in
Pregnant (warfarin is normally drug of choice for DVT)
131
Carbamazepine:
- Blocks voltage gated Na+ channels
- Trigeminal neuralgia (triggered by eating or brushing teeth)
- Carbamazepine may cause blood dyscrasias (agranulocytosis or aplastic anemia), hepatotoxicity, and SIADH
- First line for Partial Seizures and General Tonic-Clonic
132
Rifampin as Monotherapy
- rarely used alone
- Can be used as monotherapy for meningococcal exposure
- Prophylaxis for close contacts of pts with meningitis
- AMPlifies CYP450 and increases metabolism of Warfarin and Phenytoin
133
Prevent Methotrexate Toxicity w/
Folinic Acid Supplementation
134
Vincristine: Side Effect
Peripheral Neuropathy
135
Warfarin Metabolism Increased w/
antiepileptics, rifampin and griseofulvin
136
Highest risk of drug-induced SLE
Hydralazine and procainamide
137
Thiazide: Side effects
Hypercalcemia, Hyperlipidemia/hypercholesterolemia, decreased insulin release (Hyperglycemia)
138
Tx of Coagulase (-)
Usually methicillin resistant so use Vancomycin
139
Primidone
For benign essential tremors (and also tourettes)
- Active metabolite is phenobarbital and phenylethylmalonomide
- So can be useful as a narrow spectrum anticonvulsant
- Beta blockers used as first line for essential tremor but not in pts with asthma
140
Statins used with Fibrates
- Risk of myopathy with Statins increases when combined with Fibrates (eg Gemfibrozil or fenofibrate)
- Simvastatin has highest risk of myopathy
- Statins also have a risk of hepatotoxicity
141
Cocaine
- Inhibits reuptake of NE, DA, and serotonin by NET
| - Indirect sympathomimetic
142
Atropine Reversal
- Physostigmine which inhibits AchE both peripherally and centrally (due to its tertiary amine structure)
- Neostigmine and Edrophonium are also AchE inhibitors but only peripherally (they don’t cross BBB due to their quaternary amine structure)
143
Fluorinated Inhaled Anesthetics Effects
- increases cerebral blood flow but tend to depress everything else
- Can increase ICP
144
Understimulation of alpha1 receptors
lightheadedness and syncope with standing
145
Extended use of appetite suppressents
phentermine or fenfluramine are aw/ increased incidence of pulmonary hypertension → RV hypertrophy + cor pulmonale→ sudden cardiac death
146
TCAs
- inhibit reuptake of serotonin and NE
- MC cause of death is refractory hypotension and arrhythmias due to inhibition of fast Na+ channels
- can have antimuscarinic/anticholinergic effects (amytriptyline)
- may also have alpha adrenergic antagonist effects
147
Triptans
5HT1B and 5HT1D agonists (used for terminating migraines)
- induce vasoconstriction
- prevents CGRP release (vasoactive peptide)
- Don't used with CAD or prinzmetal angina
148
Loading Dose
(target concentration * Vd)/ bioavailability
149
Maintenance Dose
(target concentration * CL * interval of dosing)/bioavailability
150
Bioavailability
area under oral curve/ area under IV curve
151
Zero-order
- fixed amount eliminated
| - PEA: phenytoin, ethanol. Aspirin
152
First-order
- fixed proportion eliminated (fraction so exponential)
153
To eliminate salicylates (aspirin):
alkalinize urine w/ bicarb
154
To eliminate amphetamines:
acidify urine w/ ammonium chloride
155
Elderly Lose Phase ______ of Drug Metabolism First
Phase 1 metabolism of drugs first (CYP450)
156
Mirtazipine
alpha2 autoreceptor antagonist (atypical antidepressant)
157
Meperidine
opioid
158
Tx Glaucoma
Cholinergic promoters better
159
ACHE inhibitors
- stigmines, donepezil, galantamine, and edrophonium ( side effects of cholinergics)
- Only physostigmine crosses CNS
160
Ipratropium and Tiotropium
antimuscarinics used for asthma and COPD
161
Oxybutynin and Darefenacin
antimuscarinics used for urge incontinence
162
Scopolamine
antimuscarinic for motion sickness
163
Glycopyrrolate
antimuscarinic for preop use to decrease airway secretions, drooling, and peptic ulcer
164
Tropicamide and Atropine
Antimuscarinics used for dilation and cycloplegia
| - Atropine used for bradycardia
165
Dopamine
D1 and D2 receptors > Beta > alpha receptors
166
Dobutamine
B1 > B2, alpha (cardiac stress test)
167
Never give beta blockers to:
cocaine users (because unopposed a1 activation → severe hypertension)
168
Clonidine
- Alpha2 agonist for hypertensive emergency
- Also ethanol and opioid withdrawal
- DO NOT confuse with clomiphene (estrogen feed back inhibitor antagonist)
169
Theophylline
Bronchodilates by inhibiting PDE to increase cAMP (blocks actions of adenosine)
- Low therapeutic index (cardio and neurotoxic): seizures, arrhythmia, vomiting, abdominal pain
170
Tx for isolated systolic HTN
DHR Ca2+ Channel blockers (-dipines) or thiazides
171
Denosumab
RANKL antibody, prevents osteoclast action
172
Benzo w/ Short Half-life used for Insomnia
Triazolam
173
Amifostine
Use with platinum containing chemo agents (cisplatin) to prevent nephrotoxicity
174
Dexrazoxane
Iron chelator used with doxorubicin to prevent cardiotoxicity
175
Mesna
Used with cyclophosphamide to prevent hemorrhagic cystitis
176
Leucovorin
Used to treat methotrexate overdose
177
MRSA is resistant to:
ALL beta-lactam drugs including ones that are b-lactamase resistant (nafcillin) because it has an altered PBP
178
Nimodipine
Ca2+ Channel Blocker that ise used to prevent cerebral vasospasm following a subarachnoid hemorrhage
179
Theophylline Toxicity
Seizures and Tachyarrhythmias
180
gp41 inhibitor
enfurvitide (inhibits entry)
181
gp120 inhibitor
maraviroc (inhibits attachment)
182
Sulfahydryl group donor used to treat ________
Acetaminophen overdose
183
_______ to HIV+ Pregnant woman
Zidovudine
184
First Dose Effect w/ ACE inhibitors
First-dose hypotension
- predisposing factors: hyponatremia, hypovolemia due to diuretic use, renal impairment, heart failure, low BP, high renin or aldosterone
185
Drug Characteristics if Vd is plasma (3-5L)
high MW, high protein binding, high charge, hydrophilic
186
Piperacillin + Tazobactam is effective against:
Most Gm (-) enteric rods, including pseudomonas and Bacteroides
187
Cidofovir and Tenofovir
Nucleotides only need cellular kinase to be activated (not viral kinase)
188
T1/2=
(.693*Vd)/ CL
189
Ethosuximide
- blocks T-type Ca2+ channels
| - Used for absence seizures
190
Opioids (8)
Morphine, fentanyl, codeine, loperamide, methadone, meperidine, dextromethorphan, diphenoxylate
191
Butorphanol
Partial agonist at Mu and agonist at kappa
- analgesia for severe pain (less respiratory depression)
- Can cause withdrawal symptoms if taken with a full opioid agonist and overdose is not easily reversed
192
Tramadol
Very weak opioid agonist
- also inhibits serotonin and NE reuptake
- decreases seizure threshold, risk of Serotonin Syndrome
193
Phenytoin vs Valproic Acid Uses
Phenytoin: all seizures + status epilepticus except absence
| Valproic acid: all seizures except status epilepticus
194
Phenytoin Side effects
Nystagmus, gingival hyperplasia, hirsutism, megaloblastic anemia, fetal hydantoin (teratogen), SLE-like syndrome, p450 induction, SJS
- Zero-order Kinetics (use dependent)
195
Tx for Postherpetic neuralgia and peripheral neuropathy
Gabapentin (GABA analog that inhibits voltage gated Ca channels)
196
Barbiturates (Phenobarbital, pentobarbital, secobarbital, Thiopental)
Increased GABA duration of Cl- opening
| -contraindicated in porphyria
197
Benzodiazepines (Zolam or Zepam)
Increased GABA frequency of Cl- opening
- Short acting: triazolam, oxazepam, alprazolam, and midazolam (more likely to fall but less withdrawal)
- increased risk of falls with hangover effect
198
Short acting benzodiazepines
Triazolam
Oxazepam
Alprazolam
Midazolam
199
Nonbenzo Hypnotics
Zolpidem, Zaleplon, Eszepiclone
Act on BZ1 subtype receptor
- less dependence risk
200
Less soluble in blood -->
rapid induction and recovery
201
Inhaled Anesthetics (Halothane, -Fluranes, and NO)
Respiratory and cardiac depression, increase cerebral blood flow
- halothane has hepatotoxicity, methoxyflurane has nephrotoxicity, enflurane is proconvulsant
- Risk of malignant hyperthermia (tx w/ dantrolene)
202
IV Anesthetics
```
Barbiturates
Benzodiazepines
Ketamine
Opioids
Propafol
```
203
IV Anesthetic: Barbiturate
Thiopental: very potent and lipid soluble
- induction of anesthesia and short procedures
- rapid redistribution into tissue and fat
- decreased cerebral blood flow
204
IV Anesthetic: Benzodiazepine
Midazolam: MC used for endoscopy
- used w/ gaseous anesthetics and narcotics
- May have severe post-op respiratory depression, low BP, and anterograde amnesia
205
IV Anesthetic: Ketamine
PCP analog (dissociative anesthetic)
- Blocks NMDA receptors (decreases morphine tolerance by blocking glutamate)
- Cardio stimulant
- Causes disorientation, hallucination, and bad dreams
206
IV Anesthetic: Opioid
Morphine and fentanyl (used w/ other depressants)
207
IV Anesthetic: Propofol
Used for sedation in ICU, rapid induction, short procedures
- Less post-op nausea than thiopental
- Potentiates GABAa
208
Local Anesthetics: Esters and Amides
Esters: -Caines; Amides: Caines but w/ 2 I's
- Block Na channels (prefer activated)
- Vasoconstrictors will enhance local action
- Nerve blockade: small > large; myelin> unmyelin (size factor predominates)
- Order of Loss: pain, temp, touch, pressure
209
Bupivicaine Side Effect
Severe Cardio toxicity
210
Local Anesthetics: Infected Tissue
Need more anesthetic in infected (acidic) tissue because alkaline anesthetics can't penetrate
211
Nondepolarizing Muscular Blockade: -curium and -uronium
- competitive antagonists w/ Ach
| - Reverse with neostigmine (give w/atropine to prevent bradycardia), edrophonium, and other ACHE inhibitors
212
Dantrolene
Prevents release of Ca2+ from SR
| - Tx for malignant hyperthermia and neuroleptic malignant syndrome
213
VMAT inhibitors
Tetrabenzine and Reserpine
| - used for Huntingtons
214
D2 agonists for Parkinsons
Pramipexole and Ropinerole (non-ergots preferred) and Bromocriptine (ergot)
215
Amantadine
Antiviral that increases dopamine and can be used for Parkinsons
216
Selegiline
Selective MAO-B inhibitor for Parkinsons
217
Alzheimer's Drugs
Memantine: NMDA antagonist
| Donepezil, galantamine, rivastigmine: ACHE inhibitors
218
Benztropine
Antimuscarinic that helps with Parkinsons by curbing excess cholinergic activity
- Use for drug induced Parkinsons
219
Tx of Alcohol Withdrawal
Diazepam, Chlordiazepoxide, Disulfiram
220
Antidepressants: Risk of Inducing _______
Mania (in susceptible patients)
221
Venlafaxine
Serotonin and NE reuptake inhibitor used for PTSD
222
Pentazocine
Opioid narcotic w/ partial agonist activity and weak antagonist activity at mu receptors
- can cause withdrawal symptoms in patients dependent or tolerant to morphine/opioids
223
Alpha2 vs Beta2: insulin
A2 inhibits insulin
| B2 released insulin
224
Gancyclovir: adverse effect
Neutropenia (granulocytopenia)
| - incidence is increased with co-administration of zidovudine
225
3 types of signal pathways
cAMP, IP3, and ion channels
226
Nicotinic Receptors
Ligand gates ion channels that open after binding Ach
| - opening results in immediate influx of Na and Ca in and K out
227
Maternal to neonate HIV - prophylaxis
Zidovudone starting at 14 weeks to birth and postpartum to infant for 6 more weeks
reduced risk of transmission by 2/3s
228
DRESS Syndrome
Drug reaction 2-8 weeks after exposure
- common w/ anticonvulsants, allopurinol, sulfonamides, and antibiotics
- fever, general lymphadenopahy, facial edema, and diffuse morbilliform skin rash
- Eosinophili and atypical lymphocytosis
229
Crossing of Placenta
Water soluble materials DO NOT readily cross placenta (heparin)
Lipophilic materials easily cross (warfarin)
230
Tx for CMV Retinitis
Gancyclovir
Foscarnet
Cidofavir
231
Aciretin
synthetic retinoid used systemically to treat psoriasis
- strongly teratogenic
- retinoid medication function by binding nuclear receptors which subsequently function as transcription factors
232
Aminoglycosides used w/ Beta-lactams
Increased efficacy of aminoglycoside because beta lactam disrupts the bacterial cell wall and allows it to penetrate the bacteria and inhibit the 30S subunit
233
Orlistat
Weight loss agent for obesity
| - inhibits intestinal lipase inhibiting fat absorption in gut
234
Tx for Bullous Pemphigoid
Tetracyclines
235
ACE inhibitor fetopathy (AIF)
Blockade of angiotensin II which is needed for normal renal development
- anuria, oligohydramnios (Potters), pulmonary hypoplasia, and calvarium defects
236
Paclitaxel in a Drug Eluting Coronary Artery Stent
Functions to decrease stent thrombosis by:
inhibiting intimal hyperplasia
- binds b-tubulin and prevent microtubule break down leading to cell cycle arrest and inhibition of cell division
237
Clopidogrel w/ Omeprazole
Clopidogrel is an inactive prodrug and requires activation by CYP2C19
Omeprazole inhibits CYP2C19 causing decreased efficacy of clopidogrel
238
Nandrolone
Anabolic steroid
| - may be used in competitive atheletes
239
Jimson Weed
Mydriasis (gardener's pupil)
| Anticholinergic
240
Itraconazole
Azoles: Inhibit ergosterol synthesis by inhibiting p450
241
Fenoldopam
Used to tx Hypertensive Crisis
- Selective D1 receptor agonist
- arteriolar dilation and natriuresis (improved renal perfusion)
242
Hypertensive Emergency: Tx with ________ or _________
Fenoldopam or Nitroprusside
243
HIV Prophylaxis: Pneumocystis jirovecii and Toxoplasma Gondii
Trimethoprim-sulfamethoxazole
244
HIV Prophylaxis: MAC complex
Azithromycin
245
Norepinephrine vs Epinephrine
E: Beta more than alpha
NE: Alpha more than beta
246
Methotrexate Side Effects
Stomatitis (painful mouth ulcer), hepatotoxicity, and myelosuppression
247
Mexiletine
Class IB Antiarrhythmic
248
Propafenone
Class IC Antiarrhythmic
249
Ibutilide or Dofetilide
Class III Antiarrhythmic
250
Flecainide
Class IC Antiarrhythmic
251
Gingival Hyperplasia is a side effect of:
Phenytoin
252
Opioids and Biliary Colic
Opioid action on Mu can cause contraction of smooth muscle cells in Sphincter of oddi causing constriction and spasm --> biliary colic due to increased pressure in bile duct and gall bladder
253
PPI: Osteoporosis
Long term acid suppression w/ proton pump inhibitors --> increased risk of osteoporotic hip fractures
254
Aspirins effect on Colon Adenocarcinoma
Increased activity of COX2 is linked to some forms of colon adenocarcinoma
- aspirin use may decrease adenomatous polyp formation
255
Cilostazol
```
PDE inhibitor (direct vasodilator) and inhibits platelet aggregation
- used in patients w/ intermittent claudication
```
256
Txt for Enterococci
Vanco/amplicillin + aminoglycoside
257
Tx for Wegeners
Cyclophosphamide and Corticosteroids
258
Her2neu breast cancer
Trastuzumab
259
ER breast cancer
Tamoxifen
260
Tx for Legionella
Macrolide or Fluoroquinolone
261
Tx for Sporothrix Schenkii
Oral Potassium iodide
262
Tx for Nephrogenic DI
Amiloride, hydrochlorothiazide, indomethacin
263
Tx H Pylori
PPI + clarithromycin + amoxicillin or metronidazole
264
Tx for Ricketsia
Doxycycline
| - also Chloramphenicol
265
Tx for Chlamydia
Azithro or Doxycycline
266
Tx for Lyme
Ceftriaxone or Doxycycline
267
Tetracycline absorption inhibited by:
Milk (Ca2+), antacids (Ca+ or Mg+), or iron containing preparations
268
Tx Atypical Pneumonias w/
Macrolides or FQs
269
Binds 23 rRNA
Macrolides
| - inhibit translocation
270
Tx for Anaerobes ABOVE diaphragm
Clindamycin
271
Tx for Anaerobes BELOW diaphragm
Metronidazole
272
Sulfonamides
Inhibit folate synthesis by inhibition of dihydropteroate synthase
- hypersensitivity, hemolysis in G6PD, nephrotoxic, photosensitive, kernicterus in infants, and displaces drugs from albumin
273
Aw/ tendon rupture and arthropathy in children
Fluoroquinolones
274
Mechanism of Metronidazole
free radicals that damage DNA
275
Drug induced lupus
Isoniazid, procainamide, and hydralazine
276
Prophylaxis of Strep Pharyngitis in child w/ prior Rheumatic Fever and Prophylaxis for Endocarditis prior to dental work
Penicililn
277
Prevention of postsurgical infection w/ S. Aureus
Cefazolin
278
Prevention of gonococcal or chlamydial conjunctivitis in a newborn
Erythromycin Ointment
279
Tx for VRE (Vanco Resistant)
Linezolid or Streptogranins (-pristin)
280
Lanosterol Synthesis inhibitor
Terbinafine (inhibits squalene epoxidase)
281
Ergosterol Synthesis inhibitor
- Conazoles
| by inhibiting p450
282
Fungal Cell Wall Synthesis Inhibitor
Caspofungin
| - inhibition of b glucan
283
Fungus Membrane Pore Formation
Amphotericin B (systemic) and Nystatin (swish and swallow)
284
5FU (flucytosine)
May be used for systemic fungal infections
inhibits DNA and RNA synthesis
- bone marrow suppression
285
Mechanism of Chloroquine
Prevents detox of heme into hemozoin (heme accumulates --> toxic)
286
IFN alpha used for: (6)
Hep B and C, Kaposi, Condyloma accuminatum, Hairy cell, RCC, melanoma
287
Basiliximab
Monoclonal Ab that blocks IL2R
288
In decompensated CHF, do not use:
Beta blockers
| can be used in compensated
