Pharm Flashcards

1
Q

Km

A

inversely related to the affinity of the enzyme. Km = [S] at 1/2Vmax

if Km is bigger, means the enzyme doesn’t bind as well to the substrate, since you need more enzyme to achieve 1/2 max velocity

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2
Q

how long does it take for a drug infused at a constant rate to reach steady state?

A

4-5 half-lives

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3
Q

half-life equation

A

(0.693 x Vd) / CL

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4
Q

Clearance

A

volume of plasma cleared of drug / time

rate of drug elimination / plasma drug concentration = Vd X elimination constant

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5
Q

loading dose

A

(target plasma concentration x volume of distribution) / (bioavailability)

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6
Q

maintenance dose

A

(Cp x CL x dosage interval) / bioavailability

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7
Q

zero-order elimination + examples

A

rate of elimination constant, regardless of time. Cp dec. linearly w/ time.

Phenytoin, Ethanol, Aspirin

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8
Q

1st order elimination

A

constant fraction drug eliminated per unit time

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9
Q

competitive antagonist + example

A

1) dec. potency, but doesn’t change efficacy (shift right)

ex: diazepam + flumazenil

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10
Q

noncompetitive antagonist + examples

A

dec. efficacy –> shift curve down

ex: norepinephrine + phenoxybenzamine (note: phenoxy = irreversible competitive antagonist)

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11
Q

partial agonist

A

acts at same site as full agonist. lower efficacy –> shift down

morphine vs. buprenorphine

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12
Q

Nictoinic vs. muscarinic AcH receptors

A

1) nicotinic = ligand-gated Na/K channels

2) muscarinic = G-protein coupled receptors w/ 2nd messengers

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13
Q

Parasympathetic

A

1) cardiac + smooth muscle, gland cells, nerve terminals (muscarinic; M2 = cardiac, M3 = everywhere else)

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14
Q

Sympathetic innervation

A

1) sweat glands (muscarinic)
2) cardiac / smooth muscle: NE on alpha/beta
3) renal vasculature: D1 / D2

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15
Q

a1

A

incr:
- vascular smooth muscle
- pupillary dilator contraction
- intestinal / blader sphincter contraction

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16
Q

a2

A

dec:

  • symp. outflow
  • insulin release
  • lipolysis

incr:
-platelet aggregation

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17
Q

b1

A

incr:
- HR
- contractility
- renin release

dec. :
- lipolysis

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18
Q

b2:

A

vasodilation, bronchodilation.

incr. :
- HR
- contractility
- lipolysis
- insulin release
- aqueous humor

dec. :
- uterine tone

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19
Q

M1

A

CNS / enteric nervous system

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20
Q

M2

A

dec. HR / atrial contraction

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21
Q

M3

A

incr:

  • exocrine gland secretions (lacrimal, salivary, gastric acid)
  • gut peristalsis
  • bladder contraction / bronchoconstriction
  • pupillary sphincter contraction
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22
Q

D1

A

renal vascular smooth muscle

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23
Q

D2

A

modulates transmitter release in brain

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24
Q

H1

A

incr:

  • nasal / bronchial mucous production
  • vascular permeability

contraction of bronchioles, pruritis, pain

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25
H2
incr: | -gastric acid secretion
26
V1
Incr. vascular smooth muscle contraction
27
V2
incr. H2O permeability + reabsorption in collecting tubules of the kidney
28
Gq downstream
phospholipase C --> Dag: 1) protein kinase C 2) IP3 --> incr. ca2 --> smooth muscle contraction
29
Gs receptor mechanism
Gs --> adenylyl cyclase --> ATP conversion to cAMP --> protein kinase A --> incr. Ca2+ in heart
30
Gi receptor mechanism
inhibition of adenylyl cyclase --> ATP conversion to cAMP --> protein kinas A --> inhibition of myosin light chain kinase in smooth muscle
31
direct agonists of cholinomimetic agents
1) bethanechol 2) carbachol 3) pilocarpine 4) methacholine
32
bethanechol
1) activates bowel / bladder smoothmuscle | 2) resistant to AChe
33
carbachol:
1) glacuoma, pupillary constriction, relief of intraocular pressure
34
pilocarpine
1) stimulates sweat, tears, saliva for open / closed angle glaucoma
35
methacholine
challenge test for asthma diagnosis
36
anticholinesterases
1) neostigmine 2) pyridostigmine 3) physostigmine 4) donepezil, rivastigmine, galantamine 5) edrophonium all increase endogenous Ach
37
neostigmine
1) ileus / urinary retention, reversal of NMJ blockade (DOES NOT CROSS CNS)
38
pyridostigmine
myasthenia gravis (long acting) --> does not penetrate CNS
39
physostigmine
anticholinergic toxicity --> crosses blood-brain barrier | can fix atropine overdose
40
muscarinic antagonists
1) atropine 2) benztropine 3) scopolamine 4) ipratropium 5) oxybutynin 6) glycopyrrolate
41
atropine
muscarinic antagonist: 1) increases pupil dilation 2) dec. airway / stomach secretions 3) dec. motility 4) dec. cystitis urgency
42
epinephrine selectivity:
B > a
43
norepinephrine selectivity
a1 > a2 > B1
44
isoproterenol selectivity
B1 = B2
45
dopamine selectivity
D1 = D2 > B > a
46
dobutamine selectivity
B1 > B2
47
phenylephrine selectivity
a1 > a2
48
albuterol, salmeterol, terbutaline selectivity
B2 > B1
49
hyperglycemia as sfx drugs
``` Taking Pills Necessitates Having Blood Checked Tacrolimus Protease inhibitors Niacin HCTZ B-blocker Corticosteroid ```
50
hypothyroidism as sfx drugs
lithium amiodarone sulfonamide
51
Hepatic necrosis as sfx
``` liver "HAVAc" Halothane Amanita phalloides Valproic acid Acetaminophen ```
52
Pnacreatitis as sfx
``` Drugs Causing A Violent Abdominal Distress Didanosine Corticosteroids Alcohol Valproic acid Azathioprine Diuretics (furosemide) ```
53
Agranulocytosis as drug rxn
Drugs CCCrush Myeloblasts / Promyelocytes ``` Dapsone Clozapine Carbamazepine Colchicine Methimazole PTU ```
54
Aplastic anemia as drug rxn
Can't Make New Blood Cells Properly ``` Carbamazepine Methimazole NSAIDs Benzene Chloramphenicol PTU ```
55
Gray baby syndrome = pale skin (somewhere abroad)
chloramphenicol
56
Hemolysis in G6PD
IS D PAIN ``` INH Sulfonamide Dapsone Primaquine Aspirin Ibuprofen Nitrofurantoin ```
57
Megaloblastic anemia
PMS Phenytoin Methotrexate Sulfadrugs
58
Thrombocytopenia
Heparin | Cimetidie
59
Gingival hyperplasia drugs
phenytoin, verapamil, cyclosporin, nifedipine
60
Hyperuricemia drugs
``` Painful Tophi & Feet Need Care Pyrazinamide Thiazides Furosemide Niacin Cyclosporine ```
61
myopathy drugs
fibrates, niacin, colchicine, hydroxychloroquine, interferon-alpha, penicillamine, statins, glucocorticoids
62
photosensitivity drugs
``` SAT For Photo Sulfonamides Amiodarone Tetrayclines 5-FU ```
63
Rash / Stevens-Johnson syndrome
SJ has Epileptic Allergy to Sulfa drugs + Penicillin -anti-epileptic (ethosuximide, carbamazepine, lamotrigine, phenytoin, phenobarbital) Allopurinol Sulfa drugs Penicillin
64
SLE-syndrome drugs
``` Sulfa Hydralazine INH Procainamide Phenytoin Etanercept ```
65
Parkinson-like drugs
Cogwheel rigidity of ARM Antipsychotics Reserpine Metoclopramide
66
Seizures
``` I BITE My tongue INH (vit. B6 def) buproprion Imipenem/cilastin Tramadol Enflurane metoclopramide ```
67
SIADH drugs
Can't Concentrate Serum Sodium Carbamazepine Cyclophosphamide SSRIs
68
Pulmonary fibrosis drugs
``` Breathing Air Badly from Meds Bleomycin Amiodarone Busulfan Methotrexate ```
69
Disulfiram-like drugs
Metronidazole, cephalosporins, griseofulvin, procarbazine, 1st gen sulfonylurea
70
Nephrotoxicity / ototoxicity drugs
aminoglycosides vancomycin loop diuretics cisplatin
71
Sulfa drugs
``` Probenecid Furosemide Acetazolamide Celecoxib Thiazides Sulfonamide Sulfasalazine Sulfonylurea ```