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Rapid Fire Facts > Systems Drugs > Flashcards

Systems Drugs Flashcards

1
Q

Mech of cyclosporine

A

Binds Cyclophilin –> Complex inhibits calcineurin –> prevents IL-2 transcription

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2
Q

Uses of cyclosporine

A

Transplant rejection prophylaxis
Psoriasis
Rheumatoid arthritis

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3
Q

Cyclosporine toxicity

A 
Nephrotoxicity
HTN, Hyperlipidemia
Neurotoxicity
Gingival hyperplasia 
Hirsutism
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4
Q

Mech of Tacrolimus

A

Binds FK506BP –> complex inhibits calcineurin –> Prevents IL-2 transcription

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5
Q

uses of Tacrolimus

A

Transplant rejection prophylaxis.

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6
Q

Tacrolimus toxicity

A

Similar to cyclosporine
Increased risk of diabetes and neurotoxicity

No gingival hyperplasia or hirsutism.

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7
Q

Sirolimus mechanism

A

Binds FKBP-12 –> complex inhibits mTOR –> prevents T-cell response to IL-2

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8
Q

Sirolimus uses

A

Kidney transplant rejection prophylaxis.

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9
Q

Sirolimus toxicity

A 
Anemia
thrombocytopenia
leukopenia
insulin resistance
hyperlipidemia

non-nephrotoxic.

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10
Q

Daclizumab / Basiliximab mechanism

A

Monoclonal antibody; blocks IL-2R.

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11
Q

Daclizumab / Basiliximab uses

A

Kidney transplant rejection prophylaxis.

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12
Q

Daclizumab / Basiliximab toxicity

A

Edema, hypertension, tremor.

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13
Q

Azothioprine mechanism

A

Antimetabolite precursor of 6-mercaptopurine.

Inhibits lymphocyte proliferation by blocking nucleotide synthesis.

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14
Q

Azothioprine uses

A 
Transplant rejection prophylaxis
rheumatoid arthritis
Crohn disease
glomerulonephritis
other autoimmune conditions.
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15
Q

Azothioprine toxicity

A

Leukopenia, anemia, thrombocytopenia.

Degraded by Xanthine Oxidase - don’t give with allopurinol

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16
Q

Mycophenolate mechanism

A

Inhibits IMP dehydrogenase - decreased synthesis of guanine

Inhibits rapid proliferation of B and T cells

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17
Q

Mycophenolate toxicity

A

Hyperglycemia
hyperlipidemia
Increased risk of lymphoma and infections

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18
Q

Thalidomide mechanims

A

Suppresses TNF alpha production

Increases NK cells and IL-2

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19
Q

Thalidomide uses

A

Erythema nodosum leprosum (Hansen Disease)

Multiple myeloma

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20
Q

Thalidomide toxicity

A

Terratogen

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21
Q

Aldesleukin (IL-2) use

A

Renal cell carcinoma

Metastatic melanoma

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22
Q

Epoetin alfa (erythropoietin) use

A

Anemias (especially in renal failure)

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23
Q

Thrombopoietin

A

Thrombocytopenia

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24
Q

Oprelvekin (interleukin-11)

A

Thrombocytopenia

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25
Q

Filgrastim (G-CSF)

A

Recovery of bone marrow

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26
Q

Sargramostim (GM-CSF)

A

Recovery of bone marrow

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27
Q

INF-Alpha use

A

Chronic Hep B and C
Kaposi Sarcoma
Malignant melanoma
Hairy cell leukemia

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28
Q

IFN beta use

A

Multiple sclerosis

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29
Q

IFN gamma use

A

Chronic granulomatous disease

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30
Q

Romiplostim, eltrombopag use

A

Thrombocytopenia

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31
Q

Alemtuzumab target and use

A

CD52 –> CLL

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32
Q

Bevacizumab target and use

A

VEGF –> Colorectal cancer, renal carcinoma

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33
Q

Cetuximab target and use

A

EGFR –> Stage 4 colorectal cancer / head and neck cancer

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34
Q

Rituximab target and use

A

CD 20

B-cell non-hodgkin lymphoma
CLL
Rheumatoid arthritis
Immune thrombocytopenic purpura

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35
Q

Trastuzumab target and use

A

HER2/neu –> Breast cancer

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36
Q

Adalimumab / infliximab target and use

A

Soluble TNF alpha receptor

IBD
rheumatoid arthritis
ankylosing spondylitis
psoriasis

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37
Q

Eculizumab target and use

A

complement protein C5

Paroxysmal nocturnal hemoglobinuria

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38
Q

Natalizumab target and use

A

alpha4-integrin

Multiple sclerosis
Crohn disease

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39
Q

Abciximab target and use

A

platelet glycoproteins IIb/IIIa

prevention of ischemic complications in patients undergoing PCI

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40
Q

Denosumab target and use

A

RANKL

Osteoporosis
Inhibits osteoclast maturation

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41
Q

Digoxin immune Fab target and use

A

Antidote for digoxin toxicitiy

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42
Q

Omalizumab target and use

A

IgE

allergic asthma; prevents IgE binding to FceR1

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43
Q

Palivizumab target and use

A

RSV F-protein

RSV prophylaxis for high risk infants

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44
Q

Ranibizumab, bevacizumab target and use

A

VEGF

Neovascular age-related macular degernation

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45
Q

HMG-CoA reductase inhibitor mechanism

A

Inhibits HMG-CoA –> mevalonate

Decreases mortality in CAD patients

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46
Q

HMG-CoA reductase uses

A

Lower LDL a lot

Increased HDL

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47
Q

HMG-CoA reductase toxicities

A

Hepatotoxicity (Increased LFT)

Myopathy (esp when used with fibrates or niacin)

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48
Q

Cholestyramine, Colestipol, Colesevelam mechanism

A

Prevents intestinal reabsorption of bile acids

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49
Q

Cholestyramine, Colestipol, Colesevelam use

A

Lower LDL

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50
Q

Cholestyramine, Colestipol, Colesevelam tox

A

GI upset

Decreased absorption of other drugs and ADEK

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51
Q

Ezetimibe mechanism

A

Decreases cholesterol absorption at brush border

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52
Q

Ezetimibe uses

A

Lower LDL

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53
Q

Ezetimibe tox

A

Diarrhea

Rare LFT rise

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54
Q

Gemfibrozil, Clofibrate, Bezafibrate, Fenofibrate mechanism

A

Upregulates LPL to increase TG clearance

Activated PPAR alpha to induce HDL synth

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55
Q

Gemfibrozil, Clofibrate, Bezafibrate, Fenofibrate uses

A

Lower TAGs

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56
Q

Gemfibrozil, Clofibrate, Bezafibrate, Fenofibrate toxicity

A

myopathy (increased with statin use)

cholesterol gallstones

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57
Q

Niacin mechanism

A

Inhibits lipolysis

reduces VLDL synthesis

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58
Q

Niacin uses

A

lower LDL

Higher HDL

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59
Q

Niacin toxicity

A

Red, flushing of face (prevent with NSAID)
Hyperglycemia
Hyperuricemia

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60
Q

Opioid (Morphine, fentanyl, loperamide, methadone, meperidine, dextromethorphan, diphenoxylate, pentazocine) mechanism

A

Agonist at mu receptor - opens K+ channel, closes Ca2+ channel

Inhibits release of Ach, NE, 5-HT, glutamate, substance P

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61
Q

Dextromethorphan use

A

cough suppression

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62
Q

Loperamide, diphenoxylate use

A

Diarrhea

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63
Q

Maintenance for heroin addiction

A

Methadone

Buprenorphine + naloxone

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64
Q

Toxicity of opioids

A 
Addiction
Respiratory depression
miosis (cannot build tolerance)
constipation (cannot build tolerance)
CNS depression
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65
Q

Pentazocine mechanism

A

(Opioid) partial agonist at mu receptor + weak antagonist at mu receptor

Opioid designed to minimize addictive capacity

Can precipitate withdrawl symptoms in addicts

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66
Q

Halothane, isoflurane, sevoflurane, N2O mechanism

A

unknown

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67
Q

Halothane, isoflurane, sevoflurane, N2O effects

A

Myocardial depression
Resp depression
Nausea/emesis
Increased cerebral blood flow (decreased metabolic demand)

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68
Q

Halothane, enflurane, isoflurane, sevoflurane, methoxyflurane, N2O toxicity

A

Hepatotoxicity (Halothane)
nephrotoxicity (methoxyflurane)
Pro-convulsant (Enflurane)
Expansion of trapped gas in body cavity (N2O)

Malignant hyperthermia (all but N2O)

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69
Q

Barbiturates mechanism

A

Increases duration of Cl- channel opening in GABA neurons

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70
Q

Barbiturate uses

A

Induction of anesthesia and short surgical procedures
Sedative for anxiety
seizures
insomnia

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71
Q

How is barbiturate effect terminated?

A

Rapid redistribution into tissue (skel muscle and fat)

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72
Q

Benzodiazapine mechanism

A

Increases the frequency of Cl- channel opening in GABA neurons

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73
Q

Short acting benzos

A

Diazepam
Lorazepam
Alprozolam
Midazolam

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74
Q

Long acting benzos

A

Timazepan

Chlordiazepoxide (alcohol withdrawl)

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75
Q

Benzodiazapine toxicity

A 
severe post op resp depression
Decreased BP (treat with flumazenil)
anterograde amnesia 
Dependence 
CNS depression
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76
Q

Ketamine mechanism

A

PCP analog –> Blocks NMDA receptors

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77
Q

Ketamine toxicity

A

Disorientation
hallucination
bad dreams
Increased cerebral blood flow

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78
Q

Propofol mechanism

A

Potentiates GABA

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79
Q

Propofol use

A

IV induction agent
sedation in ICU
rapid anesthesia induction
Short procedures

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80
Q

How are the effects of propofol terminated?

A

Rapid redistribution to the rest of the body (15 min)

metabolized by liver

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81
Q

Tramadol use

A

non-addictive analgesic

Chronic pain

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82
Q

Barbiturate toxicity

A

Resp and cardio depression (fatal)
CNS depression
dependence
CYP450 inducer

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83
Q

Benzodiazapine use

A 
Anxiety
spasticity
status epilepticus (lorazepam diazepam)
Delirium tremens (EtOH withdrawl)
night terrors / sleep walking
general anesthetic
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84
Q

Zolpidem, Zaleplon, Eszopiclone mechanism

A

Non-benzo hypnotics

Act via BZ1 subtype of GABA receptor (binds GABA but not where benzo’s attach)

Short duration because of rapid metabolism by liver enzymes

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85
Q

Zolpidem, Zaleplon, Eszopiclone use

A

Insomnia

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86
Q

Zolpidem, Zaleplon, Eszopiclone toxicity

A 
Ataia 
headache
confusion
Modest day after psychomotor depression 
slight amnesia
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87
Q

Memantine mechanism

A

NMDA receptor antagonist - prevents excitotoxicity

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88
Q

Memantine use

A

Alzheimer’s Dementia

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89
Q

Memantine side effects

A

Dizziness, confusion, hallucination

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90
Q

Butorphanol mechanism

A

kappa opioid agonist and mu opioid partial agonist

analgesia

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91
Q

Butorphanol uses

A

Severe pain (migrane / labor)

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92
Q

Butorphanol toxicity

A

Opioid withdrawl symptoms if patient is also taking full opioid agonist

OD not easily reversed with naloxone.

Less respiratory depression than full opioid

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93
Q

Tramadol mechanism

A

Weak opioid agonist

Inhibits 5-HT and NE reuptake

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94
Q

Tramadol toxicity

A

Similar to opioids
Decreases seizure threshold
Serotonin syndrome

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95
Q

Ethosuximide mech

A

blocks thalamic T-type Ca channels

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96
Q

Ethosuximide uses

A

Absence seizures

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97
Q

Ethosuximide toxicity

A

GI, fatigue, headache, urticaria, Steven-Johnson syndrome.

EFGHIJ—Ethosuximide causes Fatigue, GI distress, Headache, Itching, and Stevens-Johnson syndrome

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98
Q

Phenytoin mech

A

Increases Na+ channel inactivation; zero-order kinetics

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99
Q

Phenytoin uses

A

Simple seizures
Complex seizures
Tonic-clonic seizures
Status epilepticus

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100
Q

Phenytoin toxicity

A 
Nystagmus
diplopia
ataxia
sedation
gingival hyperplasia
hirsutism
peripheral neuropathy
megaloblastic anemia
teratogenesis (fetal hydantoin syndrome) 
SLE-like syndrome
induction of cytochrome P-450
lymphadenopathy
Stevens- Johnson syndrome
osteopenia
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101
Q

Carbamazepine mech

A

Increase Na+ channel inactivation

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102
Q

Carbamazepine use

A

Simple
Complex
Tonic-clonic

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103
Q

Carbamazepine toxicity

A

Diplopia, ataxia, blood dyscrasias (agranulocytosis, aplastic anemia), liver toxicity, teratogenesis, induction of cytochrome P-450, SIADH, Stevens-Johnson syndrome

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104
Q

Valproic acid mech

A

Na+ channel inactivation, GABA concentration by inhibiting GABA transaminase

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105
Q

Valproic acid use

A

Simple
Complex
Tonic-clonic*
Absence seizures

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106
Q

Valproic acid toxicity

A

GI, distress, rare but fatal hepatotoxicity (measure LFTs), neural tube defects in fetus (spina bifida), tremor, weight gain, contraindicated in pregnancy

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107
Q

Gabapentin mech

A

Primarily inhibits high- voltage-activated Ca2+ channels; designed as GABA analog

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108
Q

Gabapentin use

A

Simple
Complex
Tonic-clonic

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109
Q

Gabapentin toxicity

A

Sedation, ataxia

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110
Q

Topiramate mech

A

Blocks Na+ channels, Increases GABA action

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111
Q

Topiramate use

A

Simple
Complex
Tonic-clonic

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112
Q

Topiramate toxicity

A

Sedation, mental dulling, kidney stones, weight loss

113
Q

Lamotrigine mech

A

Blocks voltage-gated Na+ channels

114
Q

Lamotrigine use

A

Simple
Complex
Tonic-clonic
Absence seizure

115
Q

Lamotrigine toxicity

A

Stevens-Johnson syndrome (must be titrated slowly)

116
Q

Levetiracetam mech

A

Unknown; may modulate GABA and glutamate release

117
Q

Levetiracetam use

A

Simple
Complex
Tonic-clonic

118
Q

Tiagabine mech

A

Increase GABA by inhibiting re-uptake

119
Q

Tiagabine use

A

Simple and complex seizures

120
Q

Vigabatrin mech

A

Increase GABA by irreversibly inhibiting GABA transaminase

121
Q

Vigabatrin use

A

Simple and complex seizures

122
Q

What are the local anesthetics?

A

Esters - Procaine, cocaine, tetracaine

Amides - Lidocaine, mepivicaine, bupivicaine

123
Q

Local anesthetic mech

A

Block Na+ channels by binding to specific receptors on inner portion of channel.

Preferentially bind to activated Na+ channels, so most effective in rapidly firing neurons

124
Q

Order of nerve blockade with local anesthetics

A

Small-diameter fibers > large diameter.

Myelinated fibers > unmyelinated fibers.

Overall, size factor predominates over myelination such that:

Small myelinated fibers > small unmyelinated fibers > large myelinated fibers > large unmyelinated fibers.

125
Q

Bupivicaine toxicity

A

severe cardiovascular toxicity

126
Q

Local anesthetic toxicity

A

CNS excitation, severe cardiovascular toxicity (bupivacaine), hypertension, hypotension, and arrhythmias (cocaine).

127
Q

Succinylcholine mech

A

Depolarizing NMJ blocker

Strong ACh receptor agonist; produces sustained depolarization and prevents muscle contraction.

128
Q

Succinylcholine toxicity

A

Hypercalcemia, hyperkalemia, and malignant hyperthermia.

129
Q

Tubocurarine, atracurium, mivacurium, pancuronium, vecuronium, rocuronium mechanism

A

Non-depolarizing NMJ blocker

Competitive antagonists—compete with ACh for receptors.

130
Q

Dantrolene mechanism

A

Prevents the release of Ca2+ from the sarcoplasmic reticulum of skeletal muscle.

131
Q

Baclofen mech

A

inhibits GABA(B) receptors at spinal cord level inducing skeletal muscle relaxation

132
Q

Baclofen use

A

muscle spams (acute low back pain)

133
Q

Cyclobenzaprine mech

A

Centrally acting skeletal muscle relaxant. Structurally related to TCA’s and similar anti-cholinergic side effects

134
Q

Cyclobenzaprine use

A

muscle spasm

135
Q

Bromocriptine mech

A

Ergot - Dopamine agonist (peripheral vasoconstrictor)

136
Q

Bromocriptine use

A

Parkinsons

137
Q

Pramipexol and ropinerole mech

A

Non-ergot Dopamine agonist

138
Q

Pramipexol and ropinerole use

A

Parkinsons

139
Q

Amantadine mech

A

Increase dopamine release

140
Q

Amantadine use

A

Parkinsons

141
Q

Levodopa + carbidopa mech

A

Levodopa - just L-DOPA the precursor to dopamine

Carbidopa - inhibits DOPA decarboxylase therby inhibiting peripheral conversion of L-DOPA to dopamine (L-Dopa better crosses BBB)

142
Q

Entacapone and Tolcapone mech

A

prevents peripheral L-DOPA degradation by inhibiting COMT

143
Q

Selegiline mech

A

blocks conversion of dopamine into 3-MT by selectively inhibiting MAO-B

144
Q

Selegiline toxicity

A

enhances adverse effects of L-dopa

145
Q

Levodopa/carbidopa toxicity

A

Arrhythmias from increased peripheral formation of catecholamines

Long-term use = Dyskinesia following administration, akinesia between doses
(“on-off phenomenon”)

146
Q

Tetrabenazine and Reserpine mech

A

inhibit vesicular monoamine transporter limiting dopamine vesicle packaging and release

147
Q

Tetrabenazine and Reserpine use

A

Huntington Disease

148
Q

Haloperidol mech

A

D2 receptor antagnoist

149
Q

Haloperidol use

A

Huntingtons Disease

150
Q

Sumatriptan mech

A

5-HT1B/1D agonist.

Inhibits trigeminal nerve activation

prevents vasoactive peptide release

induces vasoconstriction

Half-life

151
Q

Sumatriptan use

A

acute migrane, cluster headache attacks

152
Q

Sumatriptan toxicity

A

Coronary vasospasm (contraindicated in patients with CAD or Prinzmetal angina), mild tingling.

153
Q

Drugs safe to use in pregnancy

A

“Hypertensive Moms Love Nifedipine”

Hydralazine
Methyldopa
Labetolol
Nifidepine

154
Q

Penicillin Mech

A

Binds Penicillin binding protein (transpeptidases)

Block transpeptidase (cross-linking of peptidoglycan cell wall)

Activate autolytic enzymes

155
Q

Penicillin use

A

Mostly for Gram pos (S. pneumoniae, S. pyogenes, Actinomyces)

N. meningitidis and T. pallidum

Bactericidal for gram-positive cocci, gram-positive rods, gram-negative cocci, and spirochetes.

156
Q

Penicillin toxicity

A

Hypersensitivity reaction

Hemolytic anemia

157
Q

Penicillin resistance mech

A

penicillinase in bacteria cleaves B-lactam ring

158
Q

Ampicillin, amoxicillin (aminopenicillins) mech

A

Binds Penicillin binding protein (transpeptidases)

Block transpeptidase (cross-linking of peptidoglycan cell wall)

Wider spectrum

159
Q

Name the B-lactamase inhibitors

A

Clavulanic acid
Sulbactam
Tazobactam

160
Q

Which aminopenicillin has great oral bioavailability?

A

Amoxicillin > Ampicillin

161
Q

Ampicillin, amoxicillin (aminopenicillins) use

A

HELPSS

Haemophilus influenzae
E. coli
Listeria monocytogenes
Proteus mirabilis
Salmonella
Shigella
enterococci

Often used in UTI’s (not first line)
Neonatal infections –> E. Coli / Listeria

162
Q

Ampicillin, amoxicillin (aminopenicillins) toxicity

A

Hypersensitivity
Rash –> when given for empiric treatment of EBV mono
Pseudomembranous collitis

163
Q

Dicloxacillin, nafcillin, oxacillin mech

A

Same as penicillin (narrow spectrum)

Penicillin resistant because of bulky R group

164
Q

Dicloxacillin, nafcillin, oxacillin use

A

S. Aureus (except for MRSA)

165
Q

Dicloxacillin, nafcillin, oxacillin tox

A

Hypersensitivity reaction

Interstitial nephritis

166
Q

Piperacillin, ticaracillin mech

A

Same as penicillin

Anti-pseudomonals

Psedomonas
Gram negative rods

Give with B-lactamase inhibitors

167
Q

Cephalosporin mech

A

B-lactam drugs that inhibit cell wall synthesis
Binds PBP’s
Inhibits peptidoglycan synthesis

Less susceptible to penicillinases

Bactericidal

168
Q

Which organisms are generally not covered by cephalosporins?

A

LAME

Listeria
Atypicals (Chlamydia, Mycoplasma)
MRSA
Enterococci

169
Q

1st generation cephalosporins and uses

A

Cefazolin
Cephalexin

Gram positive cocci

PEcK
Proteus mirabilis
E. Coli
Klebsiella

170
Q

Cefazolin use

A

1st generation cephalosporin

Prior to surgery to prevent S. Aureus wound infections

171
Q

2nd generation cephalosporins and uses

A

Cefoxitin
Cefaclor
Cefuroxime

Gram positive cocci

HENS PEcK

H. Influenzae
Enterobacte aerogenes
Neisseria spp.
Serratia marcescens

Proteus Mirabilis
E. Coli
Klebsiella

172
Q

3rd generation cephalosporins and uses

A

Ceftriaxone –> meningitis, gonorrhea, Lyme
Cefotaxime
Ceftazidime –> Pseudomonas
Cefdinir –> resistant otitis media

Serious gram negative infections resistant to other B-lactams

Still covers S. Pneumo but has lost most other gram + coverage

173
Q

4th generation cephalosporin and uses

A

Cefepime

Big gun broad spectrum

Gram - organisms
Gram + organisms
Increased activity against Pseudomonas

174
Q

5th generation cephalosporin and uses

A

Broad spectrum gram + and gram - organisms

Covers MRSA
Does not cover pseudomonas

175
Q

Cephalosporin toxicity

A

Hypersensitivity reactions
autoimmune hemolytic anemia
Disulfram-like reaction with EtOH
vitamin K deficiency

Cross reactivity with penicillin

176
Q

What happens when you give a cephalosporin with an aminoglycoside?

A

Ceph increases the nephrotoxicity of aminoglycoside

177
Q

Mech of resistance against cephalosporins

A

Structural changes to the penicillin binding proteins (transpeptidase)

178
Q

Carbepenems names and mech

A

Imipenem, meropenem, Ertapenem, Doripenem

Broad spectrum, B-lactamase resistant, cell wall inhibitor

179
Q

What is a carbepenem always administered with and why?

A

Cilastin because it inhibits renal inactivation of drug in the renal tubules

Renal dihydropeptidase I

180
Q

Carbepenem use

A

Empiric treatment of life threatening disease

Gram + cocci
Gram - rods
anaerobes

181
Q

Carbepenem tox

A

GI distress
skin rash
CNS tox (seizures) at high levels

182
Q

Meropenem has which added advantage against other carbepenems?

A

Less seizure risk

stable against dehydropeptidase I in kidneys

183
Q

Aztreonam mech

A

Prevents peptidoglycan cross-linking by binding PBP3 (Penicillin binding protein 3)

Synergistic with aminoglycosides

184
Q

Can you use aztreonam in a patient allergic to penicillin?

A

yes - no cross reactivity

185
Q

Aztreonam use

A

Gram - rods only

For those who cannot tolerate aminoglycosides because of renal insufficiency

186
Q

Aztreonam toxicities

A

usually nontoxic

some GI upset

187
Q

Vanco mechanism

A

Binds D-ala D-ala portion of cell wall precursor

Bactericidal

188
Q

Vanco use

A 
Gram + bugs only -->serious MDR organisms 
MRSA
S. Epidermidis 
Enterococcus spp. 
C. Diff (oral dose)
189
Q

Vanco tox

A

NOT trouble free

Nephrotoxicity
Ototoxicity
Thrombophlebitis
Red man syndrome –> diffuse flushing

190
Q

What do you do if a patient gets red man syndrome from vanco use?

A

Withdraw drug
pre-treat with anti-histamines
slow the infusion rate

191
Q

Mech of resistance against vanco

A

Amino acid modification D-ala D-ala changed to D-ala D-lac

192
Q

What drug classes are used to treat primary (essential) HTN?

A

Thiazide
ACE I
ARBs
Dihydropyridine CCB

193
Q

What drug classes are used to treat HTN with heart failure

A

Diuretics
ACEI / ARB
B-blockers in compensated HF
Aldosterone antagonists

194
Q

What drug classes are used to treat HTN with diabetes mellitus

A

ACEI / ARB (protective against diabetic nephropathy)
CCB
Thiazides
B-blockers

195
Q

CCB names and uses

A

Amlodipine, clevidipine, nicardipine, nifedipine, nimodipine

Diltiazem, verapamil (non-dihydropyridines)

Blocks v-dependent L-type calcium channels of cardiac and smooth muscle to decrease contractility

196
Q

Dihydropyridine use

A 
HTN
Angina (including prinzmetal) 
Raynauds phenomenon 
Esophageal spasm
Migrane prophylaxis
197
Q

Nimodipine use

A

SAH (prevents cerebral vasospasm)

198
Q

Clevidipine use

A

HTN urgency or emergency

199
Q

Non-dihydropyridine use

A

HTN
Angina
A Fib / A flutter

200
Q

Non-dihydropyridine toxicity

A

Cardiac depression

AV block

201
Q

Dihydropyridine tox

A 
Peripheral edema
flushing
dizziness
hyperprolactinemia (verapamil) 
Constipation 
Gingival hyperplasia 
Reflex tachycardia
202
Q

Hydralazine mech

A

Increases cGMP –> smooth muscle relaxation

Relaxes arterioles > veins (Afterload reduction)

203
Q

Hydralazine use

A 
Severe HTN 
Heart failure (with organic nitrate)

Safe to use during pregnancy

Frequently given with B-blocker for reflex tachy

204
Q

Hydralazine tox

A

Compensatory tachycardia (contraindicated in angina/CAD)

fluid retention
headache
angina
SLE like syndrome

205
Q

Nitroprusside mech

A

short acting increase in cGMP via direct release of NO

206
Q

Nitroprusside use

A

Hypertensive emergency

207
Q

Nitroprusside tox

A

Cyanide toxicity (releases cyanide)

208
Q

Fenoldopam mech

A

D1 receptor agonist –> Coronary, peripheral, renal, and splanchnic vasodilation

Decreases BP and Increases natriuresis

209
Q

Minoxidil mech

A

opens K+ channels in smooth muscles leading to relaxation

210
Q

Minoxidil use

A

Severe HTN

211
Q

Minoxidil tox

A

Hypertrichosis
Hypotension
reflex tachy
fluid retention / edema

212
Q

Nitrate names and mech

A

Nitroglycerin, isosorbide dinitrate, isosorbide mononitrate

Increase cGMP (smooth muscle relaxation)

dilates veins&raquo_space; arteries (preload reduction)

213
Q

Nitrate use

A

angina
acute coronary syndrome
pulmonary edema

214
Q

Nitrate tox

A

Reflex tachycardia (treat with β-blockers)
hypotension
flushing
headache

215
Q

Describe industrial exposure of nitrates

A

Development of tolerance for vasodilating action during work week and loss of tolerance over the weekend

Results in tachycardia, dizziness, and headache upon re-exposure

216
Q

Which B-blockers are contraindicated in angina?

A

Pindolol
Acebutolol

Partial B-agonists

217
Q

Digoxin mech

A

Inhibits Na/K ATPase creating a smaller gradient for NCX to pump calcium out (positive inotrope)

Stimulates vagus nerve to decrease HR

218
Q

Digoxin use

A

Heart failure (increase contractility)

A Fib (decrease conduction at AV node and depression of SA node)

219
Q

Digoxin tox

A

Cholinergic — nausea, vomiting, diarrhea, blurry yellow vision (think Van Gogh).

ECG: 
Increased PR
Decreased QT
ST scooping
T-wave inversion
arrhythmia
AV block.

Hyperkalemia

220
Q

What factors predispose you to digoxin toxicity

A

renal failure (?excretion)

hypokalemia (permissive for digoxin
binding at K+-binding site on Na+/K+ ATPase)

verapamil, amiodarone, quinidine (Decreases digoxin clearance; displaces digoxin from tissue-binding sites)

221
Q

Digoxin antidote

A

slowly normalize K+
Cardiac pacer
Mg 2+
Anti-digoxin Fab fragments

222
Q

Class I anti-arrhythmics mech

A

Na channel blockers

Slow or block (decrease) conduction (especially in depolarized cells)

Decreases slope of phase 0 depolarization

State dependent (depress tissue that is frequently depolarized)

223
Q

Class IA anti-arrhythmics names and mech

A

Quinidine, Procainamide, Disopyramide

Increase AP duration
Increase ERP in ventricular action potential
Increase QT interval

224
Q

Class IA anti-arrhythmics use

A

Both atrial and ventricular arrhythmias
Re-entrant SVT
Ectopic SVT
V-Tach

225
Q

Class IA anti-arrhythmics tox

A

Cinchonism (headache, tinnitus with quinidine)

reversible SLE-like syndrome (procainamide), heart failure (disopyramide)

thrombocytopenia

torsades de pointes due to increased QT interval.

226
Q

Class IB anti-arrhythmics names and mech

A

Lidocaine, Mexiletine, Tocainide

Decrease AP duration
Slows recovery of v-gated Na channels

Preferentially affects ischemic or depolarized purkinje and ventricular tissue

Phenytoin can also fit in here

227
Q

Class IB anti-arrhythmics use

A

Acute ventricular arrhythmia (especially post MI)

Digitalis induced arrhythmia

228
Q

Class IB anti-arrhythmics to

A

CNS stimulation/depression
Cardiovascular depression

Hyperkalemia increases the toxicity of IB drugs

229
Q

Class IC anti-arrhythmics names and mech

A

Flecainide, Propafenone

Significantly prolongs ERP in AV node and accessory bypass tracts (strong Phase 0 block)

No effect on ERP in purkinje and ventricular tissues

Minimal effect on AP duration

230
Q

Class IC anti-arrhythmics use

A

SVT including A Fib

Last resort in refractory V-tach

231
Q

Class IC anti-arrhythmics tox

A

Pro-arrhythmic especially post MI

232
Q

Class II anti-arrhythmics names and mech

A

Metoprolol, propranolol, esmolol, atenolol, timolol, carvedilol

Decrease SA and AV nodal activity by decrease cAMP

Decreased Ca current

Suppress abnormal pacemakers by decreasing slope of phase 4 (slows funny current channel opening)

233
Q

Class II anti-arrhythmics use

A

SVT
ventricular rate control for A Fib
Atrial flutter

234
Q

Class II anti-arrhythmics tox

A

Impotence

exacerbation of COPD and asthma

cardiovascular effects (bradycardia, AV block, CHF)

CNS effects (sedation, sleep alterations).

May mask the signs of hypoglycemia.

Metoprolol - dylipidemia
Propranolol - exacerbate vasospasm in prinzmetal

235
Q

B-blocker overdose treatment

A

Saline
atropine
glucagon

236
Q

Class III anti-arrhythmics names and mech

A

Amiodarone, Ibutilide, Dofetilide, Sotalol

Increases AP duration
Increases ERP
Increases QT interval (slows phase 3 repol)

237
Q

Class III anti-arrhythmics use

A

A fib
a flutter
v-tach (amiodarone, sotalol)

238
Q

Class III anti-arrhythmics tox

A

Sotalol - Torsades / excessive B blockade

Ibutilide - torsades

Amiodarone: 
Pulm fibrosis 
hepatotoxicity 
hypothyroidism / hyperthyroidism
act as haptens (corneal deposits, blue/gray skin deposits resulting in photodermatitis)
neurologic effects 
constipation 
bradycardia / heart block / HF
239
Q

Class IV anti-arrhythmics names and mech

A

Verapamil, diltiazem

Decreased conduction velocity
Increased ERP
Increased PR interval
Decreased slope of phase 0 in pacemakers

240
Q

Class IV anti-arrhythmics use

A

Prevention of nodal arrythmias (SVT)

rate control in a fib

241
Q

Class IV anti-arrhythmics tox

A 
Constipation
flushing
edema
Heart failure
AV block
sinus node depression 
Torsades
242
Q

Adenosine mech

A

Increases K+ out of cells –> hyperpolarizing the cell and decreases intracellular Ca

short acting ~15 seconds

Effects blunted by theophylline and caffeine (both are adenosine receptor antagonists)

243
Q

Adenosine use

A

Drug of choice in diagnosing / abolishing supraventricular tachycardia

244
Q

Adenosine tox

A

flushing, hypotension, chest pain, sense of impending doom, bronchospasm

245
Q

Mg2+ use

A

Effective in torsades and digoxin toxicity

246
Q

H2 blockers names and mech

A

Cimetidine, ranitidine, famotidine, nizatidine

Reversible block of histamine H2-receptors

247
Q

H2 blockers use

A

Peptic ulcer, gastritis, mild esophageal reflux.

248
Q

Cimetidine tox

A

potent CYP inhibitor

antiandrogenic effects (prolactin release, gynecomastia, impotence, decreased libido in males)

Can cross BBB and placenta

Both cimetidine and ranitidine can decrease renal excretion of creatinine

249
Q

PPI names and mech

A

Omeprazole, lansoprazole, esomeprazole, pantoprazole, dexlansoprazole

Irreversibly inhibits H/K ATPase on parietal cells

250
Q

PPI uses

A

Peptic ulcer, gastritis, esophageal reflux, Zollinger-Ellison syndrome

251
Q

PPI tox

A

Increased risk of C. difficile infection
pneumonia
Hip fractures
Decreased serum Mg2+ with long-term use.

252
Q

Bismuth / sucralfate mech

A

Bind to ulcer base, providing physical protection and allowing HCO3– secretion to reestablish pH gradient in the mucous layer.

253
Q

Bismuth / sucralfate use

A

Increased ulcer healing

Traveler’s diarrhea

254
Q

Misoprostol mech

A

A PGE1 analog

Increased production and secretion of gastric mucous barrier

Decreased acid production.

255
Q

Misoprostol use

A

Prevention of NSAID induced peptic ulcers
maintain PDA
induction of labor (off-label) ripens cervix

256
Q

Misoprostol

A

Diarrhea

Contraindicated in women of childbearing potential (abortifacient) –> stimulant effect on uterus

257
Q

Octreotide mech

A

Long acting somatostatin analog

Inhibits actions of many splanchnic vasoconstriction hormones

258
Q

Octreotide

A

Acute variceal bleeds
Acromegaly
VIPoma
Carcinoid tumors

259
Q

Octreotide

A

Nausea, cramps, steatorrhea

260
Q

Antacid side effects

A

can affect absorption, bioavailability, or urinary excretion of other drugs by altering gastric and urinary pH or by delaying gastric emptying

261
Q

Aluminum hydroxide tox

A 
Constipation
Hypophosphatemia 
proximal muscle weakness
osteodystrophy
seizures
262
Q

Calcium carbonate tox

A

Hypercalcemia (stimulates gastrin release)

rebound increase in acid

263
Q

Magnesium hydroxide tox

A

Diarrhea
hyporeflexia
hypotension
cardiac arrest

264
Q

Osmotic laxative names and mech

A

Magnesium hydroxide, magnesium citrate, polyethylene glycol, lactulose

Osmotic load to draw water into GI lumen

265
Q

Osmotic laxative use

A

Constipation

Lactulose - treats hepatic encephalopathy –> gut flora degrades it into lactic acid and acetic acid –> promotes ntirogen excretion as NH4+

266
Q

Osmotic laxative tox

A

Diarrhea
dehydration
may be abused by bullimics

267
Q

Sulfasalazine mech

A

Combination of sulfapyridine (antibacterial) and 5-aminosalicylic acid (anti-inflamm)

Activated by colonic bacteria

268
Q

Sulfasalazine use

A

UC

CD

269
Q

Sulfasalzine tox

A

Malaise
nausea
sulfonamide toxicity
reversible oligospermia

270
Q

Ondansetron mech

A

5-HT3 antagonist
Decreased vagal stimulation
Powerful central-acting antiemetic.

271
Q

Ondansetron use

A

Control vomiting postoperatively and in patients undergoing cancer chemotherapy

272
Q

Ondansetron tox

A

Headache
constipation
QT interval prolongation

273
Q

Metoclopramide mech

A 
D2 receptor antagonist 
Increased resting tone of gut
Increased contractility of gut
Increased LES tone
Increased gut motility

Does not influence colon transport time

274
Q

Metoclopramide use

A

diabetic and post-OP gastroparesis

anti-emetic

275
Q

Metoclopramide tox

A

Increased parkinsonian effects
Tardive dyskinesia
Restlessness, drowsiness, fatigue, depression, nausea, diarrhea.

Drug interaction with digoxin and diabetic agents

Contraindicated in patients with small bowel obstruction or Parkinson disease (D1 receptor blockade)

276
Q

Orlistat mech

A

Inhibits gastric and pancreatic lipase

Decreases breakdown and absorption of dietary fats

277
Q

Orlistat use

A

Weight loss

278
Q

Orlistat tox

A

Steatorrhea

Decreased absorption of ADEK

Rapid Fire Facts (13 decks)

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