Pharm_Part2 Flashcards
(280 cards)
1
Q
1st generation H1 blockers
A
Diphenhydramine, dimenhydrinate, chlopheniramine Clinical uses: Allergy, motion sickness, sleep aid Toxicity: Sedation, antimuscarinic, anti-α-adrenergic
2
Q
2nd generation H1 blockers
A
Loratadine, fexofenadine, desloratadine, cetirizine (-adine) Clinical uses: Allergy Toxicity: Far less sedating than 1st generation because of ↓ entry into CNS
3
Q
ACE inhibitors: Names
A
Captopril, enalapril, lisinopril (-pril)
4
Q
Acetazolamide
A
Mechanism: Carbonic anhydrase inhibitor. Causes self-limited NaHCO3 diuresis and reduction in total-body HCO3- stores Clinical use: Glaucoma, urinary alkalinization, metabolic alkalosis, altitude sickness Toxicity: Hyperchloremic metabolic acidosis, neuropathy, NH3 toxicity, sulfa allergy
5
Q
Adalimumab
A
TNF-α inhibitors Mechanism: Anti-TNF antibody Clinical use: Rheumatoid arthritis, psoriasis, ankylosing spondylitis
6
Q
Advantages (5) & Disadvantages (4) of Oral contraception
A
Advantages: Reliable (<1% failure); ↓ risk of endometrial and ovarian cancer; ↓ incidence of ectopic pregnancy; ↓ pelvic infections; regulation of menses Disadvantages: Taken daily; No protection against STDs; ↑ triglycerides; Depression, weight gain, nausea, hypertension; Hypercoagulable state
7
Q
Albuterol
A
Asthma drug, relaxes bronchial smooth muscle (β2). Use during acute exacerbation.
8
Q
Allopurinol
A
Gout drug, chronic gout. Inhibits xanthine oxidase. ↓ conversion of xanthine to uric acid. Also used in lymphoma and leukemia to prevent tumor lysis associated urate nephropathy. ↑ concentrations of azathioprine and 6-MP (both normally metabolized by xanthine oxidase)
9
Q
Alzheimer’s drugs: Two types
A
Memantine: NMDA receptor antagonist Donepezil: Acetylcholinesterase inhibitors
10
Q
Anastrozole / exemestane
A
Aromatase inhibitors used in postmenopausal women with breast cancer
11
Q
Anesthetics - General principles: Drug with ↓ solubility in blood
A
rapid induction and recovery time
12
Q
Anesthetics - General principles: Drugs with ↑ solubility in lipids
A
↑potency = 1/MAC
13
Q
Antidote: Benzodiazepines
A
Flumazenil (competitive antagonist at GABA benzodiazepine receptor)
14
Q
Antidote: Neuromuscular blocking drugs
A
Neostigmine, edrophonium, and other cholinesterase inhibitors
15
Q
Antidote: Tricyclic antidepressants
A
NaHCO3 for CV toxicity
16
Q
Antipsychotic with low potency
A
Thioridazine, chlorpromazine - non neurologic side effects (anticholinergic, antihistamine, and α blockade effects)
17
Q
Antipsychotics (neuroleptics): Names
A
Haloperidol + “-azine”s
18
Q
Antipsychotics with high potency
A
Haloperidol, trifluoperazine, fluphenazine - neurologic side effects (extrapyramidal symptoms).
19
Q
Arachidonic acid products
A
Lipoxygenase pathway yields Leukotrienes LTB4 is a neutrophil chemotactic agent LTC4, D4, E4 function in bronchoconstriction, vasoconstriction, contraction of smooth muscle, and ↑ vascular permeability PGI2 inhibits platelet aggregation and promotes vasodilation
20
Q
Asthma drugs (7)
A
①non-specific β-agonists: Isoproterenol ②β2-agonists: Albuterol, Salmeterol ③Methylxanthines: Theophylline ④Muscarinic antagonists: Ipratropium ⑤Cromolyn ⑥Corticosteroids: Beclomethasone, prednisone ⑦Antileukotrienes: Zileuton; Zafirlukast / Montelukast
21
Q
Atypical antipsychotics: Names
A
Olanzapine, clozapine, quetiapine, risperidone, aripiprazole, ziprasidone (-apine, -idone, aripiprazole)
22
Q
Beclomethasone / prednisone
A
Asthma drug, inhibit the synthesis of virtually all cytokines. Inactivate NF-kB, the transcription factor that induces the production of TNF-α, among other inflammatory agents. 1st-line therapy for chronic asthma.
23
Q
Biphosphonates (-dronate)
A
Mechanism: Inhibit osteoclast activity; reduce both formation and resorption of hydroxyapatite Clinical use: Malignancy-associated hypercalcemia, Paget’s disease of the bone, post menopausal osteoporosis Toxicity: Corrosive esophagitis (except zoledronate), nausea, diarrhea, osteonecrosis of the jaw
24
Q
Bosentan
A
Used to treat pulmonary hypertension. Competitively antagonizes endothelin-1 receptors, decreasing pulmonary vascular resistance.
25
Bupropion
Also used for smoking cessation. ↑ NE and dopamine via unknown mechanism. Toxicity: stimulant effects (tachycardia, insomnia), headache, seizure in bulimic patients. No sexual side effects.
26
Butorphanol
Mechanism: Partial agonist at opioid mu receptors, agonist at kappa receptors. Clinical use: Pain; causes less respiratory depression than full agonists Toxicity: Causes withdraw if on full opioid agonist
27
Clinical use: ACE inhibitors
Hypertension, CHF, diabetic renal disease
28
Clinical use: Acetaminophen
Antipyretic, analgesic, but lacking anti-inflammatory properties. Used instead of aspirin to prevent Reye's syndrome in children with viral infection.
29
Clinical use: Antipsychotics
Schizophrenia (primarily positive symptoms), psychosis, acute mania, Tourette's syndrome
30
Clinical use: Aspirin
Low dose (<300 mg/day): ↓ platelet aggregation. Intermediate dose (300-2400 mg/day): antipyretic and analgesic High dose: (2400-4000 mg/day): anti-inflammatory
31
Clinical use: Atypical antipsychotics
Schizophrenia - both positive and negative symptoms
32
Clinical use: Barbiturates
Sedative for anxiety, seizures, insomnia
33
Clinical use: Benzodiazepines
Anxiety, spasticity, status epilepticus, detoxification (especially alcohol withdrawal-DTs), night terrors, sleepwalking, general anesthetic (amnesia, muscle relaxation), hypnotic (insomnia)
34
Clinical use: Buspirone
Generalized anxiety disorder. Does not cause sedation, addiction, or tolerance. Does not interact with alcohol (vs. barbiturates, benzodiazepines)
35
Clinical use: Clomipramine
OCD
36
Clinical use: COX-2 inhibitors (celecoxib)
Rheumatoid and osteoarthritis; patients with gastritis or ulcers
37
Clinical use: Duloxetine
Depression, diabetic peripheral neuropathy, duloxetine has greater effect on NE
38
Clinical use: Imipramine
Bed wetting
39
Clinical use: K+-sparing diuretics
Hyperaldosteronism, K+ depletion, CHF
40
Clinical use: Lithium
Mood stabilizer for bipolar disorder; blocks relapse and acute manic events. Also SIADH.
41
Clinical use: Monoamine oxidase (MAO) inhibitors
Atypical depression, anxiety, hypochondiasis
42
Clinical use: Nonbenzodiazepine hypnotics
Insomnia (失眠)
43
Clinical use: Olanzapine
OCD, anxiety disorder, depression, mania, Tourette's syndrome
44
Clinical use: Phenytoin
Tonic-clonic seizures. Also a class IB antiarrhythmic.
45
Clinical use: Sildenafil / vardenafil
Erectile dysfunction
46
Clinical use: SSRIs
Depression, OCD, bulimia, social phobias
47
Clinical use: Tricyclic antidepressants
Major depression, fibromyalgia
48
Clinical use: Venlafaxine
Depression, generalized anxiety disorder
49
Clomiphene
Estrogen partial agonist, partial agonist at estrogen receptors in hypothalamus. Prevents normal feedback inhibition and ↑ release of LH and FSH from pituitary, which stimulates ovulation. Used to treat infertility and PCOS. May cause hot flashes, ovarian enlargement, multiple simultaneous pregnancies, and visual disturbances
50
CNS stimulants
Methylphenidate, dextroamphetamine, mixed amphetamine salts Mechanism: ↑ catecholamines at the synaptic cleft, especially NE and dopamine Clinical use: ADHD, narcolepsy, appetite control
51
Colchicine
Gout drug, acute gout (with NSAIDs). Binds and stabilizes tubulin to inhibit polymerization, impairing leukocyte chemotaxis and degranulation. GI side effects, especially if given orally. (Note: indomethacin is less toxic, also used in acute gout)
52
Complications: Succinylcholine
Hypercalcemia, hyperkalemia, hyperthermia
53
Contraindication: Barbiturates
in porphyria
54
Contraindication: Mannitol
Anuria, CHF
55
Contraindication: Monoamine oxidase (MAO) inhibitors
with SSRI or meperidine (to prevent serotonin syndrome)
56
Contraindication: Oral contraception
smokers > 35 years of age (↑ risk of cardiovascular events), patients with history of thromboembolism and stroke or history of estrogen-dependent tumor
57
Contraindications: Estrogens
ER-positive breast cancer, history of DVTs
58
Cromolyn
Asthma drug, prevents release of mediators from mast cells. Effective only for the prophylaxis of asthma. Not effective during an acute asthmatic attack. Toxicity is rare.
59
Dantrolene
Used in the treatment of malignant hyperthermia, which is caused by inhalation anesthetics (except N2O) and succinylcholine. Also used to treat neuroleptic malignant syndrome (a toxicity of antipsychotic drugs) MOA: prevents the release of Ca2+ from the sarcoplasmic reticulum of skeletal muscle
60
Dinoprostone
PGE2 analog causing cervical dilation and uterine contraction, inducing labor
61
Diuretics: electrolyte changes: Blood pH
↓(acidemia): Carbonic anhydrase inhibitors ↑(alkalemia): Loop diuretics and thiazides
62
Diuretics: electrolyte changes: Details
Check FA2011 page475, very important mechanisms!!!
63
Diuretics: electrolyte changes: Urine Ca2+
↑Loop diuretics ↓Thiazides
64
Diuretics: electrolyte changes: Urine K+
↑ in all except K+-sparing diuretics. Serum K+ may ↓ as a result.
65
Diuretics: electrolyte changes: Urine NaCl
↑ in all diuretics. Serum NaCl may ↓ as a result.
66
DOC: 1st line for acute Status epilepsy
Benzodiazepines
67
DOC: 1st line for seizures of eclampsia
MgSO4, benzodiazepines
68
DOC: 1st line for Status epilepsy prophylaxis
Phenytoin
69
DOC: 1st line for trigeminal neuralgia
Carbamazepine
70
DOC: 1st line of epilepsy drugs in pregnant women, children
Phenobarbital
71
DOC: Acute pulmonary edema, maintenance programs for addicts
Methadone
72
DOC: ADHD
Methylphenidate (Ritalin), Amphetamines (Dexedrine)
73
DOC: Alcohol withdrawal
Benzodiazepines
74
DOC: Anorexia/bulimia
SSRI
75
DOC: Anxiety
Benzodiazepines, Buspirone, SSRI
76
DOC: Atypical depression
MAO inhibitors, SSRIs
77
DOC: Bipolar disorder
"Mood stabilizers": Lithium, Valproic acid, Carbamazepine Atypical antipsychotics
78
DOC: Closure of a PDA
Indomethacin
79
DOC: Depression
SSRIs, SNRIs, TCAs
80
DOC: Depression with insomnia
Mirtazapine
81
DOC: Diarrhea
Loperamide / Diphenoxylate
82
DOC: Essential or familial tremors
β-blockers, e.g., propranolol
83
DOC: Obsessive-compulsive disorder
SSRIs, Clomipramine
84
DOC: Pain, cough suppression
Dextromethorphan
85
DOC: Panic disorder
SSRIs, TCAs, Benzodiazepines
86
DOC: Polycystic ovarian syndrome (to prevent hirsutism)
Ketoconazole and spironolactone
87
DOC: PTSD
SSRIs
88
DOC: Schizophrenia
Antipsychotics
89
DOC: Serotonin syndrome
Cyproheptadine, 5-HT2 receptor antagonist
90
DOC: Social phobias
SSRIs
91
DOC: Tourette's syndrome
Antipsychotics (haloperidol)
92
Donepezil
Alzheimer's drugs, also galantamine, rivastigmine. Mechanism: Acetylcholinesterase inhibitors. Toxicity: Nausea, dizziness, insomnia
93
Drug class: Amiodarone
Class III antiarrhythmics
94
Drug class: Amitriptyline
Tricyclic antidepressants
95
Drug class: Amoxapine
Tricyclic antidepressants
96
Drug class: Bretylium
Class III antiarrhythmics
97
Drug class: Chlordiazepoxide
Benzodiazepines
98
Drug class: Citalopram
SSRIs
99
Drug class: Clomipramine
Tricyclic antidepressants
100
Drug class: Desipramine
Tricyclic antidepressants
101
Drug class: Dextromethorphan
Opioid analgesics for cough
102
Drug class: Diatiazem
Calcium channel blockers
103
Drug class: diaze-, -pam, -lam
Benzodiazepines
104
Drug class: Diltiazem
Class IV antiarrhythmics
105
Drug class: Disopyramide
Class IA antiarrhythmics
106
Drug class: Dofetilide
Class III antiarrhythmics
107
Drug class: Doxepin
Tricyclic antidepressants
108
Drug class: Duloxetine
SNRIs
109
Drug class: Encainide
Class IC antiarrhythmics
110
Drug class: eszopiclone
Nonbenzodiazepine hypnotics
111
Drug class: Flecainide
Class IC antiarrhythmics
112
Drug class: Fluoxetine
SSRIs
113
Drug class: Ibutilide
Class III antiarrhythmics
114
Drug class: Imipramine
Tricyclic antidepressants
115
Drug class: Isocarboxazid
MAOI
116
Drug class: Ketorolac
NSAIDs
117
Drug class: Lidocaine
Class IB antiarrhythmics
118
Drug class: methimazole
Hyperthyroidism drug
119
Drug class: Mexiletine
Class IB antiarrhythmics
120
Drug class: Naproxen
NSAIDs
121
Drug class: Nifedipine
Calcium channel blockers
122
Drug class: Nortriptyline
Tricyclic antidepressants
123
Drug class: Paroxetine
SSRIs
124
Drug class: Phenelzine
MAOI
125
Drug class: Procainamide
Class IA antiarrhythmics
126
Drug class: Propafenone
Class IC antiarrhythmics
127
Drug class: Quinidine
Class IA antiarrhythmics
128
Drug class: Selegiline
MAOI, selective MAO-B inhibitor
129
Drug class: Sertraline
SSRIs
130
Drug class: Sotalol
Class III antiarrhythmics
131
Drug class: Thiopental
Barbiturates, used for induction of anesthesia
132
Drug class: Thiopentals
Barbiturates
133
Drug class: Tocainide
Class IB antiarrhythmics
134
Drug class: Tranylcypromine
MAOI
135
Drug class: Venlafaxine
SNRIs
136
Drug class: Verapamil
Calcium channel blockers
137
Drug class: Zaleplon
Nonbenzodiazepine hypnotics
138
Drug class: Zolpidem (Ambien)
Nonbenzodiazepine hypnotics
139
Drug use: Pirenzepine
Muscarinic antagonist
140
Drug use: Propantheline
Muscarinic antagonists
141
Epilepsy drug toxicities: Diplopia, ataxia, blood dyscrasias (agranulocytosis, aplastic anemia), liver toxicity, teratogenesis, induction of cytochrome P-450, SIADH, Stevens-Johnson syndrome
Carbamazepine
142
Epilepsy drug toxicities: Ethosuximide
EFGH - Ethosuximide, Fatigue, GI, Headache
143
Epilepsy drug toxicities: GI distress, fatigue, headache, urticaria, Stevens-Johnson syndrome
Ethosuximide
144
Epilepsy drug toxicities: GI distress, rare but fetal hepatotoxicity (measure LFTs), neural tube defects in fetus (spina bifida), tremor, weight gain. Contraindicated in pregnancy.
Valproic acid
145
Epilepsy drug toxicities: Nystagmus, diplopia, ataxia, sedation, gingival hyperplasia, hirsutism, megaloblastic anemia, teratogenesis (fetal hydantoin syndrome), SLE-like syndrome, induction of cytochrome P-450
Phenytoin
146
Epilepsy drug toxicities: Sedation, tolerance, dependence
Benzodiazepines
147
Epilepsy drug toxicities: Sedation, tolerance, dependence, induction of cytochrome P-450
Phenobarbital
148
Estrogens (ethinyl estradiol, DES, mestranol)
Mechanism: Bind estrogen receptors Clinical use: Hypogonadism or ovarian failure, menstrual abnormalities, HRT in postmenopausal women; use in men with androgen-dependent prostate cancer. Toxicity: ↑ risk of endometrial cancer, bleeding in postmenopausal women, ↑ risk of thrombi
149
Etanercept
TNF-α inhibitors Mechanism: Recombinant form of human TNF that binds TNF (Decoy receptor) Clinical use: Rheumatoid arthritis, psoriasis, ankylosing spondylitis
150
Ethacrynic acid
Mechanism: Phenoxyacetic acid dericative (NOT a sulfonamide). Essentially same action as furosemide. Clinical use: Diuresis in patients allergic to sulfa drugs Toxicity: Similar to furosemide; can be used in hyperuricemia, acute gout (never used to treat gout)
151
Evolution of EPS side effects
4h acute dystonia (muscle spasm, stiffness, oculogyric crisis) 4d akinesia (parkinsonian symptoms) 4wk akathisia (restlessness) 4mo tardive dyskinesia
152
Expectorants (2)
Guaifenesin: Expectorant - removes excess sputum; does not suppress cough reflex. N-acetylcysteine: Mucolytic - can loosen mucous plugs in CF patients. Also used as an antidote for acetaminophen overdose.
153
Fetal hydantoin syndrome
Intrauterine growth restriction with microcephaly and develop minor dysmorphic craniofacial features and limb defects including hypoplastic nails and distal phalanges (birth defects).
154
Finasteride (Propecia)
a 5α-reductase inhibitor (↓ conversion of testosterone to dihydrotestosterone). Useful in BPH. Also promotes hair growth - used to treat male-pattern baldness
155
Flutamide
a nonsteroidal competitive inhibitor of androgens at the testosterone receptor. Used in prostate carcinoma.
156
Furosemide
Mechanism: Sulfonamide loop diuretic. Inhibits cotransport system (Na+, K+, 2Cl-) of thick ascending limb of loop of Henle. Abolishes hypertonicity of medulla, preventing concentration of urine. ↑Ca2+ excretion Clinical use: Edematous states (CHF, cirrhosis, nephrotic syndrome, pulmonary edema), hypertension, hypercalcemia
157
Glaucoma drugs: Cholinomimetics
Direct: Pilocarpine, carbachol Indirect: Physostigmine, echothiophate
158
Glaucoma drugs: Diuretics
Acetazolamide, dorzolamide (-zolamide)
159
Glaucoma drugs: Emergencies
Pilocarpine
160
Glaucoma drugs: Prostaglandin
Latanoprost (PGF2α)
161
Glaucoma drugs: α-agonists
Epinephrine, Brimonidine
162
Glaucoma drugs: β-blockers
Timolol, betaxolol, carteolol
163
Hormone replacement therapy (HRT)
Used for relief or prevention of menopausal symptoms (e.g., hot flashes, vaginal atrophy) and osteoporosis (↑estrogen, ↓osteoclast activity) Unopposed estrogen replacement therapy (ERT) ↑ the risk of endometrial cancer, so progesterone is added. Possible ↑ CV risk
164
Huntington's drugs
Disease: ↑dopamine, ↓GABA+ACh Reserpine + tetrabenazine - amine depleting Haloperidol - dopamine receptor antagonist
165
Hydrochlorothiazide
Mechanism: Thiazide diuretic. Inhibits NaCl reabsorption in early distal tubule, reducing diluting capacity of the nephron. ↓ Ca2+ excretion Clinical use: Hypertension, CHF, idiopathic hypercalciuria, nephrogenic diabetes insipidus Toxicity: Hypokalemic metabolic alkalosis, hyponatremia, hyperglycemia, hyperlibidemia, hyperuricemia, and hypercalcemia. Sulfa allergy
166
Infliximab
TNF-α inhibitors Mechanism: Anti-TNF antibody Clinical use: Crohn's disease, rheumatoid arthritis, ankylosing spondylitis Toxicity: Predisposes to infections (reactivation of latent TB)
167
Intravenous anesthetics: Arylcyclohexylamines (Ketamine)
PCP analogs that act as dissociative anesthetics. Block NMDA receptors. Cardiocascular stimulants. Cause disorientation, hallucication, and bad dreams. ↑cerebral blood flow.
168
Intravenous anesthetics: Barbiturates
Thiopental - high potency, high lipid solubility, rapid entry into brain. Used for induction of anesthesia and short surgical procedures. Effect terminated by rapid redistribution into tissue and fat. ↓cerebral blood flow.
169
Intravenous anesthetics: Benzodiazepines
Midazolam most common drug used for endoscopy; used adjunctively with gaseous anesthetics and narcotics. May cause severe postoperative respiratory depression, ↓BP (treat overdose with flumazenil), and amnesia
170
Intravenous anesthetics: Opiates
Morphine, fentanyl used with other CNS depressants during general anesthesia
171
Intravenous anesthetics: Propofol
Used for rapid anesthesia induction and short procedures. Less postoperative nausea than thiopental. Potentiates GABA(A).
172
Ipratropium
Asthma drug, competitive block of muscarinic receptors, preventing bronchoconstriction. Also used for COPD, with ↓ production of mucus.
173
Isoproterenol
Asthma drug, relaxes bronchial smooth muscle (β2). Adverse effect is tachycardia (β1).
174
K+-sparing diuretics: Names
Spironolactone, Triamterene, Amiloride, Eplerenone
175
Latanoprost
PGF2α, ↑outflow of aqueous humor Side effects: Darkens color of iris (browning)
176
Leuprolide
Mechanism: GnRH analog with agonist properties when used in pulsatile fasion; antagonist properties when used in continuous fasion Clinical use: Infertility (pulsatile), prostate cancer (continuous - use with flutamide), uterine fibroids Toxicity: Antiandrogen, nausea, vomiting
177
Local enesthetics: Two groups
Esters - procaine, cocaine, tetracaine Amides - Lidocaine, mepivacaine, bupivacaine (amides have 2 i's in name)
178
Losartan
an angiotensin II receptor antagonist. It is not an ACE inhibitor and does not cause cough.
179
Mannitol
Mechanism: Osmotic diuretic, ↑tubular fluid osmolarity, producing ↑ urine flow Clinical use: Shock, drug overdose, ↑intracranial / intraocular pressure Toxicity: Pulmonary edema, dehydration
180
Maprotiline
Blocks NE reuptake. Toxicity: sedation, orthostatic hypotension.
181
Mechanism: ACE inhibitors
Inhibit angiotensin-converting enzyme, reducing levels of angiotensin II and preventing inactivation of bradykinin, a potent vasodilator. Renin release is ↑ due to loss of feedback inhibition
182
Mechanism: Acetaminophen
Reversibly inhibits cyclooxygenase, mostly in the CNS. Inactivated peripherally.
183
Mechanism: Antipsychotics
All typical antipsychotics block dopamine D2 receptors (↑[cAMP]1)
184
Mechanism: Aspirin
Irreversibly inhibit cyclooxygenase (both COX-1 and COX-2). Block prostaglandin synthesis.
185
Mechanism: Benzodiazepines
Facilitate GABA(A) action by ↑frequency of Cl- channel opening. ↓REM sleep. Most have long half-lives and active metabolites
186
Mechanism: Buspirone
Stimulates 5-HT1A receptors
187
Mechanism: COX-2 inhibitors (celecoxib)
Reversibly inhibit specifically the cyclooxygenase (COX) isoform 2, which is found in inflammatory cells and vascular endothelium and mediates inflammation and pain; spares COX-1, which helps maintain the gastric mucosa. Thus, should not have the corrosive effects of other NSAIDs on the GI lining.
188
Mechanism: L-dopa/carbidopa
↑level of dopamine in brain. Unlike dopamine, L-dopa can cross blood-brain barrier and is converted by dopa decarboxylase in the CNS to dopamine
189
Mechanism: Lithium
Possibly related to inhibition of phosphoinositol cascade
190
Mechanism: Local anesthetics
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. 3° amine local anesthetics penetrate membrane in uncharged form, then bind to ion channels as charged form
191
Mechanism: Monoamine oxidase (MAO) inhibitors
Nonselective MAO inhibition ↑ levels of amine neurotransmitters (NE, serotonin, dopamine)
192
Mechanism: Nonbenzodiazepine hypnotics
Act via the BZ1 receptor subtype and is reversed by flumazenil
193
Mechanism: Selegiline
Selectively inhibites MAO-B, which preferentially metabolizes dopamine over NE and 5-HT, thereby increasing the availability of dopamine
194
Mechanism: Sildenafil / vardenafil
Inhibit cGMP phosphodiesterase, causing ↑ cGMP, smooth muscle relaxation in the corpus cavernosum, ↑ blood flow, and penile erection. Sildenafil and vardenafil fill the penis.
195
Mechanism: SNRIs
Inhibit serotonin and NE reuptake
196
Mechanism: Spironolactone
a competitive aldosterone receptor antagonist in the cortical collecting tubule
197
Mechanism: SSRIs
Serotonin-specific reuptake inhibitors
198
Mechanism: Triamterene / Amiloride
act at the cortical collecting tubule by blocking Na+ channels in the DCT
199
Mechanism: Tricyclic antidepressants
Block reuptake of NE and serotonin
200
Memantine
Alzheimer's drug Mechanism: NMDA receptor antagonist; helps prevent excitotoxicity (mediated by Ca2+) Toxicity: Dizziness, confusion, hallucinations
201
Mifepristone (RU-486)
Mechanism: Competitive inhibitor of progestins at progesterone receptors Clinical use: Termination of pregnancy. Administered with misoprostol (PGE1) Toxicity: Heavy bleeding, GI effects (nausea, vomiting, anorexia), abdominal pain
202
Mirtazapine
α2 antagonist (↑ release of NE and serotonin) and potent 5-HT2 and 5-HT3 receptor antagonist. Toxicity: sedation, ↑ appetite, weight gain, dry mouth.
203
MOA: Atypical antipsychotics
Block 5-HT2, dopamine, α, and H1 receptors
204
MOA: Barbiturates
Facilitate GABA(A) action by ↑duration of Cl- channel opening, thus ↓neuron firing
205
MOA: Carbamazepine
↑Na+ channel inactivation
206
MOA: Ethosuximide
Blocks thalamic T-type Ca2+ channels
207
MOA: H1 blockers
Reversible inhibitors of H1 histamine receptors
208
MOA: Ketoconazole
Inhibits steroid synthesis (inhibits desmolase)
209
MOA: Opioids analgesics
Act as agonists at opioid receptors (mu=morphine, delta=enkephalin, kappa=dynorphin) to modulate synaptic transmission - open K+ channels, close Ca2+ channels → ↓synaptic transmission. Inhibit release of ACh, NE, 5-HT, glutamate, substance P
210
MOA: Phenytoin
Use-dependent blockade of Na+ channels; ↑refractory period; inhibition of glutamate release from excitatory presynaptic neuron
211
MOA: Spironolactone
Inhibits steroid binding
212
MOA: Valproic acid
↑Na+ channel inactivation, ↑GABA concentration
213
Molecular: GABA(A)-R
A ligand-gated chloride channel binded by benzos, barbs, and EtOH
214
Monitoring: Lithium
Narrow therapeutic window requires close monitoring of serum levels. Almost exclusively excreted by the kidneys; most is reabsorbed at the proximal convoluted tubules following Na+ reabsorption
215
Monoamine oxidase (MAO) inhibitors: Names
Phenelzine, tranylcypromine, isocarboxazid, selegiline (selective MAO-B inhibitor)
216
Name Inhaled anesthetics (3)
Halothane, -flurane, nitrous oxide
217
Neuroleptic malignant syndrome (NMS)
rigidity, myoglobinuria, autonomic instability, hyperpyrexia. Treatment: dantrolene, D2 agonists (e.g., bromocriptine) FEVER: Fever, Encephalopathy, Vitals unstable, Elevated enzymes, Rigidity of muscles
218
Neuromuscular blocking drugs: Two groups
Depolarizing: Succinylcholine Nondepolarizing: Tubocurarine, -curium, -curonium
219
NSAIDs
Ibuprofen, naproxen, indomethacin, ketorolac Mechanism: Reversibly inhibit cyclooxygenase (both COX-1 and COX-2). Block prostaglandin synthesis. Clinical use: Antipyretic, analgesic, anti-inflammatory. Toxicity: Renal damage, fluid retention, aplastic anemia, GI distress, ulcers.
220
Order of nerve blockade: Local anesthetics
Small myelinated fibers > Small unmyelinated fibers > Large myelinated fibers > Large unmyelinated fibers
221
Parkinson's disease drugs: Four groups
Agonize dopamine receptors: a.ergot: Bromocriptine b.non-ergot: pramipexole ropinirole ↑dopamine: Amantiadine, L-dopa/carbidopa Prevent dopamine breakdown: Selegiline, -capone Curb excess cholinergic activity: Benztropine
222
Principle: Local anesthetics in acidic tissue
In infected (acidic) tissue, alkaline anesthetics are charged and cannot penetrate membrane effectively. More anesthetic is needed in these cases.
223
Probenecid
Gout drug, chronic gout. Inhibits reabsorption of uric acid in PCT (also inhibits secretion of penicillin)
224
Progestins
Mechanism: Bind progesterone receptors, reduce growth, and ↑ vascularization of endometrium Clinical use: Used in oral contraceptives and in the treatment of endometrial cancer and abnormal uterine bleeding
225
Raloxifene
Estrogen partial agonist, agonist on the bone; reduces resorption of bone; used to treat osterporosis
226
Reason: Why not use salicylates to treat gout?
All but the highest doses depress uric acid clearance. Even high doses (5-6 g/day) have only minor uricosuric activity
227
Ritodrine / Terbutaline
β2-agonists that relax the uterus; reduce premature uterine contractions
228
Salmeterol
Asthma drug, long-acting agent for prophylaxis. Adverse effects are tremor and arrhythmia.
229
Seizures: Almost always from temporal lobe (mood changes, illusions, hallucinations); impaired consciousness and postictal state are present
Complex partial, DOC: Carbamazepine
230
Seizures: Brief arrhythmic jerking movements, last < 1 sec, usually occur in clusters for a few minutes; no loss of consciousness
Myoclonic, DOC: Valproic acid
231
Seizures: Brief episode of staring, but no postictal confusion
Absence, DOC: Ethosuximide, valproate
232
Seizures: Generalized tonic extension of the extremities, followed by clonic rhythmic movements; loss of consciousness and prolonged postictal confusion are present
Tonic-clonic, DOC: Phenytoin, carbamazepine, and valproate
233
Seizures: One body part is involved; no loss of consciousness and no postictal confusion
Simple partial, DOC: Carbamazepine
234
Serotonin syndrome
Hyperthermia, myoclonus, cardiovascular collapse, flushing, diarrhea, seizures
235
Short acting benzodiazepines (3)
Triazolam, Oxazepam, Midazolam → Highest addictive potential
236
Side effects: Tricyclic antidepressants
Sedation, α-blocking effects, atropine-like side effects. 3° TCAs (amitriptyline) have more anticholinergic effects than do 2° TCAs (nortriptyline). Desipramine is the least sedating and has lower seizure threshold.
237
SNRIs: Names
Venlafaxine, duloxetine
238
SSRIs: Names
Fluoxetine, paroxetine, sertraline, citalopram
239
Steven-Johnson syndrome
Prodome of malaise and fever followed by rapid onset of erythmatous / purpuric macules (oral, ocular, genital). Skin lesions progress to epidermal necrosis and sloughing
240
Sumatriptan
Mechanism: 5-HT(1B/1D) agonist. Causes vasoconstriction, inhibition of trigeminal activation and vasoactive peptide release. Half-life < 2 hours Clinical use: Acute migraine, cluster headache attacks. Toxicity: Coronary vasospasm (contraindicated in patients with CAD or Prinzmetal's angina), mild tingling
241
Tamoxifen
Estrogen partial agonist, antagonist on the breast tissue; used to treat and prevent recurrence of ER-positive breast cancer
242
Tamsulosin
α1-antagonist used to treat BPH by inhibiting smooth muscle contraction. Selective for α1(A,D) receptors (found in prostate) vs. vascular α1(B) receptors
243
Tardive dyskinesia
stereotypic oral-facial movements due to long-term antipsychotic use. Often irreversible.
244
Testosterone (methyltestosterone)
Mechanism: Agonist at androgen receptors Clinical use: Treat hypogonadism and promote development of 2° sex characteristics; stimulation of anabolism to promote recovery after burn or injury; treat with ER-positive breast cancer (exemastane) Toxicity: Causes masculinization in females; reduces intratesticular testosterone in males by inhibiting release of LH (via negative feedback), leading to gonadal atrophy. Premature closure of epiphyseal plates. ↑LDL, ↓HDL
245
Theophylline
Asthma drug, likely causes bronchodilation by inhibiting phosphodiesterase, thereby ↓ cAMP hydrolysis. Usage is limited because of narrow therapeutic index (cardiotoxicity, neurotoxicity); metabolized by P-450. Blocks actions of adenosine.
246
Toxicity: ACE inhibitors
Cough, Angioedema, Proteinuria, Taste changes, hypOtesion, Pregancy problems, Rash, Increased renin, Lower angiotensin II. CAPTOPRIL. Also, hyperkalemia. Avoid with bilateral renal artery stenosis because ACE inhibitors significantly ↓ GFR by preventing constriction of efferent arterioles
247
Toxicity: Acetaminophen
Overdose produces hepatic necrosis; acetaminophen metabolite depletes glutathione and forms toxic tissue adducts in liver. N-acetylcysteine is antidote - regenertates glutathione.
248
Toxicity: Antipsychotics
1. Highly lipid soluble and stored in body fat; thus, very slow to be removed from body. 2. Extrapyramidal system (EPS) side effects. 3. Endocrine side effects (e.g., dopamine receptor antaganism → hyperprolactinemia → galactorrhea) 4. Side effects arising from blocking muscarinic (dry mouth, constipation), α (hypotension), and histamine (sedation) receptors. 5. Neuroleptic malignant syndrome (NMS) / Tardive dyskinesia
249
Toxicity: Aspirin
Gastric upset. Chronic use can lead to acute renal failure, interstitial nephritis, and upper GI bleeding. Reye's syndrome in children with viral infection.
250
Toxicity: Atypical antipsychotics
Fewer extrapyramidal and anticholinergic side effects than traditional antipsychotics
251
Toxicity: Barbiturates
Dependence, additive CNS depression effects with alcohol, respiratory or cardiovascular depression (can lead to death), drug interactions owing to induction of liver microsomal enzymes (cytochrome P-450)
252
Toxicity: Benzodiazepines
Dependence, additive CNS depression effects with alcohol. Less risk of respiratory depression and coma than with barbiturates
253
Toxicity: Bupivacaine
CNS excitation, severe cardiovascular toxicity
254
Toxicity: Chlorpromazine
Corneal deposits
255
Toxicity: Clozapine
may cause agranulocytosis
256
Toxicity: Cocaine
Hypertension, hypotension, and arrhythmias
257
Toxicity: COX-2 inhibitors (celecoxib)
↑ risk of thrombosis. Sulfa allergy. Less toxicity to GI mucosa (lower incidence of ulcers, bleeding than NSAIDs)
258
Toxicity: Enflurane
Proconvulsant
259
Toxicity: Halothane
Hepatotoxicity
260
Toxicity: K+-sparing diuretics
Hyperkalemia (can lead to arrhythmias), endocrine effects with aldosterone antaganists (e.g., spironolactone causes gynecomastia, antiandrogen effects)
261
Toxicity: L-dopa/carbidopa
Arrhythmias from peripheral conversion to dopamine. Long-term use can → dyskinesia following administration, akinesia between doses. Carbadopa, a peripheral decarboxylase inhibitor, is given with L-dopa in order to ↑ the bioavailability of L-dopa in the brain and to limit peripheral side effects
262
Toxicity: Lithium
Tremor, sedation, edema, heart block, hypothyroidism, polyurea (ADH antagonist causing nephrogenic diabetes insipidus). Fetal cardiac defects include Ebstein anomaly and malformation of the great vessels.
263
Toxicity: Methoxyflurane
Nephrotoxicity
264
Toxicity: Monoamine oxidase (MAO) inhibitors
Hypertensive crisis with tyramine ingestion (in many foods, such as wine and cheese) and β-agonists; CNS stimulation.
265
Toxicity: Nitrous oxide
Expansion of trapped gas
266
Toxicity: Nonbenzodiazepine hypnotics
Ataxia, headaches, confusion. Shorter duration because of rapid metabolism by liver enzymes. Unlike older sedative-hypnotics, cause only modest day-after psychomotor depression and few amnestic effects. Lower dependence risk than benzodiazepines
267
Toxicity: Olanzapine / Clozapine
may cause significant weight gain
268
Toxicity: Opioid analgesics
Addiction, respiratory depression, constipation, miosis (pinpoint pupils), additive CNS depression with other drugs. Tolerance does not develop to miosis and constipation.
269
Toxicity: Phenytoin
Nystagmus, ataxia, diplopia, sedation, SLE-like syndrome, induction of cytochrome P-450. Chronic use produces gingival hyperplasia in children, peripheral neuropathy, hirsutism, megaloblastic anemia (↓folate absorption). Teratogenic (fetal hydantoin syndrome).
270
Toxicity: Selegiline
May enhance the adverse effects of L-dopa
271
Toxicity: Sildenafil / vardenafil
Headache, flushing, dyspepsia, impaired blue-green color vision. Risk of life-threatening hypotension in patients taking nitrates.
272
Toxicity: SNRIs
↑ BP most common; also stimulant effects, sedation, nausea
273
Toxicity: SSRIs
Fewer than TCAs. GI distress, sexual dysfunction (anorgasmia). "Serotonin syndrome" with any drug that ↑ serotonin (e.g., MAO inhibitors)
274
Toxicity: Thioridazine
Retinal deposits
275
Toxicity: Tricyclic antidepressants
Tri-C's: Convulsions, Coma, Cardiotoxicity (arrhythmias); also respiratory depression, hyperpyrexia. Confusion and hallucinations in elderly due to anticholinergic side effects.
276
Tramadol
Mechanism: Very weak opioid agonist; also inhibits serotonin and NE reuptake (works on multiple neurotransmitters - "tram it all" in) Clinical use: Chronic pain Toxicity: Similar to opioids. Decreases seizure threshold
277
Trazodone
Primarily inhibits serotonin reuptake. Used for insomnia, as high doses are needed for antidepressant effects. Toxicity: sedation, nausea, priapism, postural hypotension.
278
Tricyclic antidepressants: Names
Imipramine, amitriptyline, desipramine, nortriptyline, clomipramine, doxepin, amoxapine (-ipramine, -triptyline, doxepin, amoxapine)
279
Zafirlukast, montelukast
block leukotriene receptors. Especially good for aspirin-induced asthma.
280
Zileuton
A 5-lipoxygenase pathway inhibitor. Blocks conversion of arachidonic acid to leukotrienes
