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Flashcards in PHARM LOTS! Deck (223):
1

Common side effect of hypnotic agents

Sedation

2

Occurs when sedative hypnotics are used chronically or at high doses

Tolerance

3

The most common type of drug interaction of sedative hypnotics with other depressant medications

Additive CNS depression

4

Major effect of benzodiazepines on sleep at high doses

REM is decreased

5

Neurologic SE of benzodiazepines

Anterograde amnesia

6

Reason benzos are used cautiously in pregnancy

Ability to cross the placenta

7

Main route of metabolism for benzodiazepines

Hepatic

8

Benzodiazepine that undergo extrahepatic conjugation (which are useful in older or hepatically impaired)

Lorazepam, oxazepam, and temazepam

9

MOA for benzodiazepines

increase the FREQUENCY of GABA-mediated chloride ion channel opening

10

Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects)

Flumazenil

11

Benzodiazepine with useful relaxant effects in skeletal muscle spasticity of central origin

Diazepam

12

Benzodiazepine that has efficacy against absence seizures and in anxiety states, such as agoraphobia

Clonazepam

13

Benzodiazepines that are the most effective in the treatment of panic disorder

Alprazolam and Clonazepam

14

Benzodiazepine that is used for anesthesia

Midazolam

15

DOC for status epilepticus

Diazepam

16

Longer acting benzodiazepines used in the management of withdrawal states of alcohol and other drugs

Chlordiazepoxide and Diazepam

17

Agents having active metabolites, long half lives, and a high incidence of adverse effects

Diazepam, Flurazepam, chlordiazepoxide, and clorazepate

18

Barbiturates may precipitate this hematologic condition

Acute intermittent porphyria

19

Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetics property

Liver enzyme INDUCTION

20

Barbiturates MOA

Increase the DURATION of GABA-mediated chloride ion channels

21

Barbiturate used for the induction of anesthesia

Thiopental

22

Important drug interaction with chloral hydrate

May displace coumadin from plasma proteins

23

Site of action for zaleplon and zolpidem

Benzodiazepine receptor BZ1 (although are not considered benzodiazepines)

24

Good hypnotic activity with less CNS SE than most benzodiazepines

Zolpidem, zaleplon

25

Agent that is a partial agonist for the 5-HT1A receptor

Buspirone

26

Drug of choice for generalized anxiety disorder, NOT effective in acute anxiety

Buspirone

27

Agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS)

Ethanol

28

Agent with zero-order kinetics

Ethanol, theophylline, tolbutamide, warfarin, aspirin, phenytoin

29

Rate limiting step of alcohol metabolism

Aldehyde dehydrogenase

30

System that increases in activity with chronic exposure and may contribute to tolerance

Microsomal ethanol oxidizing system (MEOS)

31

Enzyme that metabolizes acetaldehyde to acetate

Aldehyde dehydrogenase

32

Agents that inhibit aldehyde dehydrogenase

Disulfiram, metronidazole, certain sulfonylureas and cephalosporins

33

Agent used in the treatment of alcoholism, if alcohol is consumed concurrently, acetaldehyde builds up and results in nausea, headache, flushing, and hypotension

Disulfiram

34

The most common neurologic abnormality in chronic alcoholics

Peripheral neuropathy (also excessive alcohol use is associated with HTN, anemia, and MI)

35

Agent that is teratogen and causes a fetal syndrome

Alcohol

36

Agent that competes for alcohol dehydrogenase in the case of methanol overdose

Ethanol

37

Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure

Fomepizole

38

Most frequent route of metabolism

Hepatic enzymes

39

Mechanisms of action for Phenytoin, Carbamazepine, Lamotrigine

Sodium blockade

40

MOA for benzodiazepines and barbiturates

GABA-related targets

41

MOA for Ethosuximide

Calcium channels

42

MOA for Valproic acid at high doses

Affect calcium, potassium, and sodium channels

43

Drugs of choice for generalized tonic-clonic and partial seizures

Valproic acid, Phenytoin and Carbamazepine

44

DOC for febrile seizures

Phenobarbital

45

Drugs of choice for absence seizures

Ethosuximide and valproic acid

46

Drug of choice for myoclonic seizures

Valproic acid

47

Drugs of choice for status epilepticus

IV diazepam (or lorazapam) followed by phenytoin

48

Drugs that can be used for infantile spasms

Corticosteroids

49

Anti-seizure drugs used also for bipolar affective disorder (BAD)

Valproic acid, carbamazepine, phenytoin and gabapentin

50

Anti-seizure drugs used also for Trigeminal neuralgia

Carbamazepine

51

Anti-seizure drugs used also for pain of neuropathic orgin

Gabapentin

52

Anti-seizure agent that exhibits non-linear metabolism, highly protein bound, causes fetal hydantoin syndrome, and stimulates hepatic metabolism

Phenytoin

53

SE of phenytoin

Gingival hyperplasia, nystagmus, diplopia and ataxia

54

Anti-seizure agent that induces formation of liver drug-metabolism enzymes, is teratogen and can cause craniofacial anomalies and spina bifida

Carbamazepine

55

Agent that inhibits hepatic metabolism, is hepatotoxic and teratogen that can cause neural tube defects and gastrointestinal distress

Valproic acid

56

Laboratory value required to be monitored for patients on valproic acid

Serum ammonia and LFT's

57

SE for Lamotrigine

Stevens-Johnson syndrome

58

SE for Felbamate

Aplastic anemia and acute hepatic failure

59

Anti-seizure medication also used in the prevention of migraines

Valproic acid

60

Carbamazepine may cause

Agranulocytosis

61

Anti-seizure drugs used as alternative drugs for mood stabilization

Carbamazepine, gabapentin, lamotrigine, and valproic acid

62

MOA of general anesthetics

Unclear, thought to increase the threshold for firing of CNS neurons

63

Inhaled anesthetic with a low blood/gas partition coefficient

Nitrous oxide

64

Inversely related to potency of anesthetics

Minimum alveolar anesthetic concentration (MAC)

65

Inhaled anesthetics metabolized by liver enzymes which has a major role in the toxicity of these agents

Halothane and methoxyflurane

66

Most inhaled anesthetics SE

Decrease arterial blood pressure

67

Inhaled anesthetics are myocardial depressants

Enflurane and halothane

68

Inhaled anesthetic causes peripheral vasodilation

Isoflurane

69

Inhaled anesthetic that may sensitize the myocardium to arrhythmogenic effects of catecholamines and has produced hepatitis

Halothane

70

Inhaled anesthetics, less likely to lower blood pressure than other agents, and has the smallest effect on respiration

Nitrous oxide

71

Fluoride released by metabolism of this inhaled anesthetic may cause renal insufficiency

Methoxyflurane

72

Prolonged exposure to this inhaled anesthetic may lead to megaloblastic anemia

Nitrous oxide

73

Pungent inhaled anesthetic which leads to high incidence of coughing and vasospasm

Desflurane

74

DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics

Dantrolene

75

IV barbiturate used as a pre-op anesthetic

Thiopental

76

Benzodiazepine used adjunctively in anesthesia

Midazolam

77

Benzodiazepine receptor antagonist, it accelerates recovery from benzodiazepine overdose

Flumazenil

78

This produces "dissociative anesthesia", is a cardiovascular stimulant which may increases intracranial pressure, and hallucinations occur during recovery

Ketamine

79

Opioid associated with awareness during surgery and post-operative recall, but still used for high-risk cardiovascular surgeries

Fentanyl

80

State of analgesia and amnesia produced when fentanyl is used with droperidol and nitrous oxide

Neuroleptanesthesia

81

Produces both rapid anesthesia and recovery, has antiemetic activity and commonly used for outpatient surgery, may cause marked hypotension

Propofol

82

MOA of local anesthetics (LA's)

Block voltage-dependent sodium channels

83

This may enhance activity of local anesthetics

Hyperkalemia

84

This may antagonize activity of local anesthetics

Hypercalcemia

85

Almost all local anesthetics have this property and sometimes require the administration of vasoconstrictors (ex. Epinephrine) to prolong activity

Vasodilation

86

Local anesthetic with vasoconstrictive property, favored for head, neck, and pharyngeal surgery

Cocaine

87

Longer acting local anesthetics which are less dependent on vasoconstrictors

Tetracaine and bupivacaine

88

These LA's have surface activity

Cocaine and benzocaine

89

Most important toxic effects of most local anesthetics

CNS toxicity

90

Commonly abused LA which has cardiovascular toxicity including severe hypertension with cerebral hemorrhage, cardiac arrhythmias, and myocardial infarction

Cocaine

91

LA causing methemoglobinemia

Prilocaine

92

Structurally related to acetylcholine, used to produce muscle paralysis in order to facilitate surgery or artifical ventilation. Full doses lead to respiratory paralysis and require ventilation

Neuromuscular blocking drugs

93

These drugs strongly potentiate and prolong effect of neuromuscular blockade (NMB)

Inhaled anesthetics, especially isoflurane, aminoglycosides, and antiarrhythmic

94

These prevent the action of ACh at the skeletal muscle endplate to produce a "surmountable blockade," effect is reversed by cholinesterase inhibitors (ex. neostigmine or pyridostigmine)

Nondepolarizing type antagonists

95

Agent with long duration of action and is most likely to cause histamine release

Tubocurarine

96

Non-depolarizing antagonist has short duration

Mivacurium

97

Agent can block muscarinic receptors

Pancuronium

98

Agent undergoing Hofmann elimination (breaking down spontaneously)

Atracurium

99

One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis, causes muscle pain postoperatively and myoglobinuria may occur

Succinylcholine

100

During Phase I these agents worsen the paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine

Cholinesterase inhibitors

101

Agents acting in the CNS or in the skeletal muscle, used to reduce abnormally elevated tone caused by neurologic or muscle end plate disease

Spasmolytic drugs

102

Facilitates GABA presynaptic inhibition

Diazepam

103

GABA agonist in the spinal cord

Baclofen

104

Similar to clonidine and may cause hypotension

Tizanidine

105

DOC for malignant hyperthermia by acting on the sarcoplasmic reticulum or skeletal muscle

Dantrolene

106

Agent used for acute muscle spasm

Cyclobenzaprine

107

Antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog) and is irreversible

Drug induced Parkinsonism

108

Agent used in drug therapy of Parkinson's instead of Dopamine which has low bioavailability and does not cross the BBB

L-dopa

109

This is combined with L-dopa, inhibits DOPA decarboxylase (active only peripherally) which allows lower effective doses of L-dopa and allows for fewer SE's (GI distress, postural hypotension, and dyskinesias)

Carbidopa

110

Clinical response that may fluctuate in tx of Parkinson's dx

"On-off-phenomenon"

111

Anti-Parkinson's drug which increases intraocular pressure and is contraindicated in closed angle glaucoma

Levodopa

112

Ergot alkaloid that is a partial agonist at D2 receptors in the brain, used for patients who are refractory or cannot tolerate levodopa, causes erythromelalgia

Bromocriptine

113

Non ergot agents used as first-line therapy in the initial management of Parkinson's

Pramipexole and ropinirole

114

Enhances dopaminergic neurotransmission SE's include CNS excitation, acute toxic psychosis and livedo reticularis

Amantadine

115

Inhibitor of MAO type B which metabolizes dopamine, used adjunct to levodopa or as sole agent in newly diagnosed pt's

Selegiline

116

Inhibitors of catechol-O-methyltransferase (COMT), used as adjuncts in Parkinson's dx and cause acute hepatic failure (monitor LFT's)

Entacapone and Tolcapone

117

Agent decreases the excitatory actions of cholinergic neurons. May improve tremor and rigidity but have LITTLE effect on bradykinesia. Atropine-like side effects

Benztropine

118

Agent effective in physiologic and essential tremor

Propranolol

119

Agents used in Huntington's Disease

Tetrabenazine (amine depleting drug), Haloperidol (antipsychotic)

120

Agents used in Tourette's dx

Haloperidol or pimozide

121

Chelating agent used in Wilson's disease

Penicillamine

122

Extrapyramidal dysfunction is more common with these agents, which block this subtype of dopamine receptor

Older antipsychotic agents, D2 receptors

123

Side effects occuring in antipsychotics that block dopamine

EPS, hyperprolactinemia, amennorrhea, galactorrhea, neuroleptic malignant syndrome

124

Antipsychotics that reduce positive symptoms only

Older antipsychotics

125

Newer atypical antipsychotics that also improve some of the negative symptoms and help acute agitation

Olanzapine and aripiprazole

126

Atypical antipsychotic causing high prolactin levels

Risperidone

127

Newer atypical antipsychotic used for bipolar disorder, known to cause weight gain, and adversely affect diabetes

Olanzapine

128

Agent more frequently associated with extrapyramidal side effects that can be treated with benzodiazepine, diphenhydramine or muscarinic blocker

Haloperidol

129

Drug used in neuroleptic malignant syndrome

Dantrolene

130

Agents may exacerbate tardive dyskinesias (may be irreversible and there is no treatment)

Muscarinic blockers

131

Antipsychotics having the strongest autonomic effects

Chlorpromazine or Thioridazine

132

Antipsychotic having the weakest autonomic effects

Haloperidol

133

Only phenothiazine not exerting antiemetic effects, can cause visual impairment due to retinal deposits, and high doses have been associated with ventricular arrhythmias

Thioridazine

134

Agent with greater affinity to 5HT2A receptor; reserved for refractory schizophrenia, and can cause weight gain and agranulocytosis

Clozapine

135

Anti-psychotics shown not to cause tardive dyskinesia

Clozapine and quetiapine

136

Anti-psychotics available in depot preparation

Fluphenazine and haloperidol

137

Reduced seizure threshold

Low-potency typical antipsychotics and clozapine

138

Orthostatic hypotension and QT prolongation

Low potency and risperidone

139

Increased risk of developing cataracts

Quetiapine

140

Major route of elimination for Lithium

Kidneys

141

Patients being treated with lithium, who are dehydrated, or taking diuretics concurrently, could develop

Lithium toxicity, lithium-induced nephrogenic diabetes insipidus

142

Drug increases the renal clearance hence decreases levels of lithium

Theophylline

143

Lithium is associated with this congenital defect

Cardiac anomalies; contraindic: pregnancy&lactation

144

DOC for bipolar affective disorder

Lithium

145

SE of lithium

Tremor, sedation, ataxia, aphasia, thyroid enlargement, and reversible diabetes insipidus

146

Example of three antidepressants that are indicated for obsessive compulsive disorder

Clomipramine, fluoxetine and fluvoxamine

147

Neurotransmitters affected by the action of antidepressants

Norepinephrine and serotonin

148

Usual time needed for full effect of antidepressant therapy

2 to 3 weeks

149

Population group especially sensitive to side effects of antidepressants

Elderly patients

150

All antidepressants have roughly the same efficacy in treating depression, agents are chosen based on these criterion

Side-effect profile and prior pt response

151

Well-tolerated and are first-line antidepressants

SSRI's, bupropion, and venlafaxine

152

Most useful in patients with significant anxiety, phobic features, hypochondriasis, and resistant depression

Monamine oxidase inhibitors

153

Condition will result from in combination of MAOI with tyramine containing foods (ex. wine, cheese, and pickled meats)

Hypertensive crisis

154

MAOI should not be administered with SSRI's or potent TCA's due to development of this condition

Serotonin syndrome

155

Sedation is a common side effect of these drugs, they lower seizure threshold, uses include BAD, acute panic attacks, phobias, enuresis, and chronic pain and their overdose can be deadly

Tricyclic antidepressants (TCA)

156

Three C's associated with TCA toxicity

Coma, Convulsions, Cardiac problems (arrhythmias and wide QRS)

157

Agents having higher sedation and antimuscarinic effects than other TCA's

Tertiary amines

158

TCA used in chronic pain, a hypnotic, and has marked antimuscarinic effects

Amitriptyline

159

TCA used in chronic pain, enuresis, and OCD

Imipramine

160

TCA with greatest sedation of this group, and marked antimuscarinic effects, used for sleep

Doxepin

161

TCA used in obsessive compulsive disorder (OCD), most significant of TCA's for risk of seizure, weight gain, and neuropsychiatric signs and symptoms

Clomipramine

162

Secondary amines that have less sedation and more excitation effect

Nortriptyline, Desipramine

163

Antidepressant associated with neuroleptic malignant syndrome

Amoxapine

164

Antidepressant associated with seizures and cardiotoxicity

Maprotiline

165

Antidepressant having stimulant effects similar to SSRI's and can increase blood pressure

Venlafaxine

166

Antidepressant inhibiting norepinephrine, serotonin, and dopamine reuptake

Venlafaxine

167

Antidepressant also used for sleep that causes priapism

Trazodone

168

Antidepressant which is inhibitor of CYP450 enzymes and may be associated with hepatic failure

Nefazodone

169

Unicyclic antidepressant least likely to affect sexual performance, used for management of nicotine withdrawal, SE's include dizziness, dry mouth, aggravation of psychosis, and seizures

Bupropion

170

Antidepressant with MOA as alpha 2 antagonist, has effects on both 5-HT and NE, blocks histamine receptors, and is sedating

Mirtazapine

171

SE of mirtazapine

Liver toxicity, increased serum cholesterol

172

Except for these agents all SSRI have significant inhibition of CytP450 enzymes

Citalopram and its metabolite escitalopram

173

SSRI with long T1/2 and can be administered once weekly for maintenance, not acute tx

Fluoxetine

174

SSRI indicated for premenstrual dysphoric disorder

Fluoxetine (Sarafem)

175

Some of SSRIs' therapeutic effects beside depression

Panic attacks, social phobias, bulimia nervosa, and PMDD (premenstrual dysphoric disorder), OCD

176

SSRI's less likely to cause a withdrawal syndrome

Fluoxetine

177

Inhibit synaptic activity of primary afferents and spinal cord pain transmission neurons

Ascending pathways

178

Activation of these receptors close Ca2+ ion channels to inhibit neurotransmitter release and pain transmission

Presynaptic mu, delta, and kappa receptors

179

Activation of these receptors open K+ ion channels to cause membrane hyperpolarization

Postsynaptic Mu receptors

180

Tolerance to all effects of opioid agonists can develop except

Miosis, convulsions and constipation

181

All opioids except this agent (which has a muscarinic blocking action) cause pupillary constriction

Meperidine

182

SE of these drugs include dependence, withdrawal syndrome, sedation, euphoria, respiratory depression nausea and vomiting, constipation, biliary spasm, increased ureteral and bladder tone, and reduction in uterine tone

Opioid Analgesics

183

Strong opioid agonists

Morphine, methadone, meperidine, and fentanyl

184

Opioids used in anesthesia

Morphine and fentanyl

185

Opioid used in the management of withdrawal states

Methadone

186

Opioid available trans-dermally

Fentanyl

187

Opioid that can be given PO, by epidural, and IV, which helps to relieve the dyspnea of pulmonary edema

Morphine

188

Use of this opioid with MAOI can lead to hyperpyrexic coma, and with SSRI's can lead to serotonin syndrome

Meperidine

189

Moderate opioid agonists

Codeine, hydrocodone, and oxycodone

190

Weak opioid agonist, poor analgesic, its overdose can cause severe toxicity including respiratory depression, circulatory collapse, pulmonary edema, and seizures

Propoxyphene

191

Partial opioid agonist, considered a strong analgesic, has a long duration of action and is resistant to naloxone reversal

Buprenorphine

192

Opioid antagonist that is given IV and had short DOA

Naloxone

193

Opioid antagonist that is given orally in alcohol dependency programs

Naltrexone

194

These agents are used as antitussive

Dextromethorphan, Codeine

195

These agents are used as antidiarrheal

Diphenoxylate, Loperamide

196

Inhalant anesthetics

NO, chloroform, and diethyl ether

197

Toxic to the liver, kidney, lungs, bone marrow, peripheral nerves, and cause brain damage in animals, sudden death has occurred following inhalation

Fluorocarbons and Industrial solvents

198

Cause dizziness, tachycardia, hypotension, and flushing

Organic nitrites

199

Causes acne, premature closure of epiphyses, masculinization in females, hepatic dysfunction, MI, and increases in libido and aggression

Steroids

200

Readily detected markers that may assist in diagnosis of the cause of a drug overdose include

Changes in heart rate, blood pressure, respiration, body temperature, sweating, bowel signs, and pupillary responses

201

Most commonly abused in health care professionals

Heroin, morphine, oxycodone, meperidine and fentanyl

202

This route is associated with rapid tolerance and psychologic dependence

IV administration

203

Lacrimation, rhinorrhea, yawning, sweating, weakness, gooseflesh, nausea, and vomiting, tremor, muscle jerks, and hyperpnea are signs of this syndrome

Abstinence syndrome

204

Treatment for opioid addiction

Methadone, followed by slow dose reduction

205

This agent may cause more severe, rapid and intense symptoms (abstinence syndrome) to a recovering addict

Naloxone

206

Sedative-Hypnotics action

Reduce inhibition, suppress anxiety, and produce relaxation

207

Additive effects when Sedative-Hypnotics used in combination with these agents

CNS depressants

208

Common mechanism by which overdose result in death

Depression of medullary and cardiovascular centers

209

"Date rape drug"

Flunitrazepam (rohypnol)

210

The most important sign of withdrawal syndrome

Excessive CNS stimulation (seizures)

211

Treatment of withdrawal syndrome involves

Long-acting sedative-hypnotic or a gradual reduction of dose, clonidine or propranolol

212

These agents are CNS depressants

Ethanol, Barbiturates, and Benzodiazepines

213

Withdrawal from this drug causes lethargy, irritability, and headache

Caffeine

214

W/D from this drug causes anxiety and mental discomfort

Nicotine

215

Treatments available for nicotine addiction

Patches, gum, nasal spray, psychotherapy, and bupropion

216

Chronic high dose abuse of nicotine leads to

Psychotic state, overdose causes agitation, restlessness, tachycardia, hyperthermia, hyperreflexia, and seizures

217

Tolerance is marked and abstinence syndrome occurs

Amphetamines

218

Amphetamine agents

Dextroamphetamines and methamphetamine

219

These agents are congeners of Amphetamine

DOM, STP, MDA, and MDMA "ecstasy"

220

Overdoses of this agent with powerful vasoconstrictive action may result in fatalities from arrhythmias, seizures, respiratory depression, or severe HTN (MI and stroke)

Cocaine "super-speed"

221

Most dangerous of the currently popular hallucinogenic drugs, OD leads to nystagmus, marked hypertension, and seizures, presence of both horizontal and vertical nystagmus is pathognomonic

PCP

222

Removal of PCP may be aided

Urinary acidification and activated charcoal or continual nasogastric suction

223

THC is active ingredient, SE's include impairment of judgment, and reflexes, decreases in blood pressure and psychomotor performance occur

Marijuana