General Flashcards Preview

Pharmacology Block 2 > General > Flashcards

Flashcards in General Deck (274)
Loading flashcards...
1

Phenytoin

-AE
-Na blocker
-long term pot hirtuism and osteoporosis
-marked confusion (cognitive impairment), teratogen
-cause gingival hyperplasia in 20%
-hard to regulate

2

Tiagabine

-AE
-incr GABA-- reuptake inh (prolong chanel open)
-adjunct in partial seizures
-short half life

3

Rufinamide

-AE Na channel blocker
-add on for lenox-gastaut syndrome

4

Valporic acid

(divalporex) broad spectrum AE
-Treats all seizures- FIRST LINE
-teratogen, osteoporosis, weight gain, hair loss, hepatic and pancreatic injury
-cyp inducer
-also treats bipolar

5

Perampanel

AMPA antag AE
-partial seizures and tonic-clonic

6

Tonic-clonic seizure

Initial strong contraction of whole musculature; followed by series of violent jerks that gradually die out (2-4 min).

7

Which AE's cause cognitive impairment?

Phenobarbital, phenytoin and topiramate

8

Lamotrigine

-Broad spectrum AE (alt to valproic acid -- less SE) prolong inact Na and inh glut
-FIRST LINE general
-tonic clonic seizures and lenox-gastaut
-Rash when dose incr too rapidly

9

Vigabatrin

-AE
Irrev inh GABA-T (GABA aminotransferase)-- degr enzyme
-patrial seizures
-RARELY used -- vision loss

10

Ezogabine

-AE
enhance K channels (KCNQ family)

11

Which AEs cause osteoporosis

Phenytoin, phenobarbital, carbamazepine, oxcarbazepine and valproic acid.

12

Ethosuxamide

-AE that decr Ca
-Absent seizures (FIRST LINE)

13

Felbamate

-AE
-Broad spectrum-- multiple mechs (NMDA antag and enhance GABA)
-aplastic anemia

14

Carbamazepine

-AE Na channel blocker
-modulate sustained high freq firing
-Autoinduction (incr clearance with incr dose)
-osteoporosis and teratogen

15

Which AEs are teratogenic?

Valproic acid & carbamazepine; barbiturates & phenytoin. Newer AEDs less teratogenic.

16

Leviteracetam

-AE that binds to SV2A
-Broad spectrum (modify release of GABA and glut)
-not many SEs

17

Clonazepam

-Long acting BZD--- AE
-incr GABA
-sedation, memory impair, mood changes, addiction.
-also used in anxiety and panic

18

Non-linear drug clearance

Either clearance decreases as dose increases or clearance increases with dose increase.
-with AEs

19

Topirimate

-Broad spectrum AE
-memory impair, renal stones, glaucoma, weight loss

20

Gabapentin and pregabalin

-AE that binds alpha-2-delta of Ca channel --- decr glut
-unsteadiness, weight gain, fatigue, dizzy
-also for neuropathic pain, chronic pain, fibromyalgia

21

What is a seizure?

a group of cortical neurons that discharge abnormally

22

phenobarbital

-AE enhance GABA
-weak acid-- elim by making urine alkaline
-similar to penytoin (preferred)
cognitive impair, osteoporosis, sedation
-not for absence

23

List 3 highly selective nonergot derivatives (dopamine agonist)

1. Pramipexole
2. Ropinirole
3. Apomorphine
Fewer side effects and are therefore preferred.

24

What are the 3 categories of partial seizures?

Simple
Complex
Secondarily Generalized

25

Most AED's cause some CNS depression, therefore, what other drugs should be avoided?

Etoh, antihistamines, other AED's, opioids.

26

How effective is Memantine?

Only modest benefit

27

How is preclinical AD diagnosed?

Completely on the basis of biomarkers

28

What is tegretol indicated for?

Like phenytoin, partial seizures and tonic-clonic seizures.

29

What is the first line drug class of choice for mild to moderate PD motor symptoms?

Dopamine agonists

30

What are the principal adverse effects of levodopa?

nausea, dyskinesia, hypotension, and psychosis.

31

If combined with levodopa, what drug will cause a hypertensive crisis?

MAOI

32

Which two AED's have the highest risk of causing suicidality?

Topamax and Lamictal

33

What is the unique side effect caused by phenytoin in 20% of patients?

gingival hyperplasia

34

How can you minimize the risk to the fetus?

Use one drug at the lowest possible dose and avoid Depakote

35

What is the name of the enzyme that converts levodopa to dopamine?

decarboxylase

36

What is the primary pathology in PD?

Degeneration of neurons in the substantia nigra that supply dopamine to the striatum. The result is an imbalance between dopamine and acetylcholine.

37

Which COMT is safer and therefore preferred?

Entacapone

38

Name the 4 cholinesterase inhibitors that are approved for AD.

1. Donepezil
2. Galantamine
3. Rivastigmine
4. Tacrine

39

What is the gold standard for treatment of PD motor symptoms?

Levodopa + carbidopa

40

How are the motor symptoms of Parkinson's Disease treated best?

Primarily with dopamine agonists. Anticholinergics can also be used.

41

Tegretol is often better tolerated than phenytoin, therefore, it is often preferred. True of False?

T

42

Rarely, phenytoin causes SJS or toxic epidermal necolysis (TEN). What may increase the risk?

HLA-B1501 gene variation, seen almost exclusively in pts of Asian descent.

43

What are the categories of generalized seizures?

Tonic-Clonic (Grand Mal)
Absence (Petit Mal)
Atonic
Myoclonic
Status Epiletpticus
Febrile

44

What role do NMDA receptors play?

learning and memory

45

How does carbidopa enhance the effects of levodopa in PD?

By preventing decarboxylation of levodopa in the intestine and peripheral tissues. (Can't cross blood-brain barrier, so does not prevent conversion of levodopa to dopamine in the brain.)

46

What is a COMT drug and how do they work?

Catechol O-methyltransferase (COMT) inhibitors inhibit metabolism of levodopa in the periphery resulting in raised dopamine levels in treating PD.

47

How do you treat AD dementia?

Cholinesterase inhibitors or memantine (Namenda).
Benefit in most patients is marginal.

48

Dopamine agonists do have more serious side effects than levodopa. List some.

Hallucinations
Sleepiness
Postural hypotension
*Usually reserved for younger patients who can tolerate better.

49

What is the major known risk factor in developing AD?

Advancing age

50

What are the 2 major adverse reactions with Depakote?

1. Potentially fatal liver injury (espec children

51

What is phenytoin indicated for?

Partial seizures and tonic-clonic seizures. NOT absence seizures.

52

What is the new class of drugs for AD?

NMDA receptor antagonists. Memantine (Namenda) is the first representative. Benefits are derived from modulating the effects of glutamate at NMDA receptors.

53

How does levodopa work to relieve motor symptoms in PD?

Levodopa relieves motor symptoms by converting to dopamine in surviving nerve terminals in the striatum and restores a proper balance between dopamine and AcH.

54

Depakote is a very broad spectrum AED. What are it's indications?

ALL seizure types including most generalized seizures - tonic-clonic, absence, atonic, and myoclonic sz's.

55

Dopamine agonists fall into two groups. What are they?

1. Ergot derivatives
2. Nonergot derivatives

56

How long do you treat AD?

Indefinitely, or until the SE's are intolerable or benefits are lost.

57

How do the MAO-B Inhibitors enhance responses to levodopa?

By inhibiting MAO-B, the brain enzyme that inactivates dopamine.

58

Only 1 cholinesterase inhibitor is approved for treating severe AD. Which one is it?

Donepezil

59

What is gabapentin used for?

Partial seizures, restless leg syndrome, phantom limb pain, and neurogenic pain.

60

What are the 2 MAO-B Inhibitors used with levodopa in treating PD?

1. Selegiline
2. Rasagiline

61

What are the 2 COMT drugs?

1. Entacapone
2. Tolcapone

62

What is the histology of Alzheimers (AD)?

Characterized by: 1. neuritic plaques 2. neurofibrillary tangles 3. degeneration of cholinergic neurons in the hippocampus and cerebral cortex.

63

How would you treat status epilepticus?

Initially, IV diazepam or lorazepam. Follow with Phenytoin if seizures do not stop. Move onto phenobarbital IV until stops.

64

When is the oral nonergot dopamine agonist, pramipexole indicated?

Alone in early PD for motor symptoms or with levodopa in advanced PD

65

What are the 3 phases of AD?

1. An asymptomatic preclinical phase
2. Two symptomatic clinical phases:
a). Mild cognitive impairment
b) Dementia - both due to AD.

66

What is PD

A neurodegenerative disorder that produces characteristic motor symptoms: tremor at rest, rigidity, postural instability, and bradykinesia.

67

What are neuritic plaques?

Spherical, extracellular bodies that consist of a beta-amyloid core surrounded by remnants of axons and dendrites.

68

PD affects the ____

basal ganglia

69

What is the dopamine content of the substantia niagra in PD patients?

less than 10% of normal in PD patient brains postmortem

70

MPTP

is a compound used experimentally to study Parkinson's disease; it impairs dopaminergic neurons

71

A molecule aspect of PD involves ______

Lewy bodies in various parts of the brain

72

Alpha synuclein

staining used to reveal Lewy bodies

73

Genetic forms of PD ____ and _______

PARK7 and PINK1

74

Main DE of LDOPA

Dyskinesias and a rapid fluctuation in clinical state

75

Acute side effects of LDOPA

Nausea, anorexia, hypotension

76

Bromocriptine

PD
-Primarily dopamine agonist; used most often in cases of hyperprolactinemia

77

Pergolide & cobergoline

PD
-dopamine agonist

78

Pramipexole and Ropinirole

-PD
D2/3 selective dopamine agonists, better tolerated; no fluctuations in efficacy

79

Rotigotine

Newer dopamine agonist, delivered as a transdermal patch
-PD

80

Apomorphine

-PD
Dopamine agonist with a powerful emetic action; must be combined with an antiemetic; LAST RESORT COMPOUND

81

Seligiline

-PD
MAO-B inhibitor (selective), used in combination with levodopa

82

Tolcapone and entacopone

Catechol-O-Methyltransferase inhibitors; used with L-DOPA and never alone

83

Deep brain stimulation

in PD
-electrode is placed into the subthalamic nucleus; used in cases where patients are intolerant to medication

84

Orphenadrine

Muscarinic receptor antagonist used for the parkinsonism caused by antipsychotic drugs

85

Amantadine

May enhance dopamine release

86

What is HD?

An inherited (autosomal dominant) disorder resulting in progressive brain degeneration

87

Trinucleotide repeat

in Huntington's disease this expansion of the number of repeats of the CAG sequence coding for glutamine is over 50

88

Which drugs treat the invol movements of HD?

Tetrabenazine and chlorpromazine; baclofen

89

Baclofen

GABA agonist in HD

90

Tetrabenazine

-HD
Inhibitor of monoamine transporter 2 (VMAT2); decreases dopamine levels in addition to serotonin and norepi.

91

Amyloid cascade hypothesis

in AD
-Amyloid precursor protein accumulates following processing, aggregating to form plaques that are thought to damage the brain.

92

An allelic variant of apolipoprotein-E (APOE)-E4

Associated with 20 % of sporadic and familial AD; making it the single most important risk factor

93

Highly selective and reversible AChE inhibitor used in AD

Donepezil

94

Rivastigmine

-AD
Inhibits both AChE and butryylcholinesterase. Transdermal patch allows once a day administration and fewer GI side effects.

95

Galantamine

-AD
Reversible and competitive inhibitor of AChE and also an allosteric modulator binding to cholinergic nicotinic receptors.

96

Memantine

Noncompetitive glutamatergic receptor antagonist, blocking/regulating NMDA receptors

97

Cognitive reserve

Maximized by increasing social circle, maintaining a healthy weight, cognitively stimulating activities and strong literary skills

98

Pathophysio of AD

Acetylcholine in the diffuse cortex

99

Most prominent side effect of tricyclic antidepressants

anticholinergic

100

Tyrosine hydroxylase

Rate limiting enzyme in dopamine synthesis

101

Mertazapine

Atypical antidepressant with adverse effects of somnolence, increased appetite, weight gain, constipation and dizziness

102

Paroxetine

SSRI most assoc with constipation

103

Sertraline

SSRI most assoc with diarrhea

104

Buproprion

Atypical antidepressant used to treat depression and smoking cessation

105

These MAO-I potentially causes the most drug-food interactions

MAO-A selective

106

Serotonin syndrome

Due to high levels of serotonin; usually a drug interaction, and consists of hyperthermia, muscle rigidity, and fluctuations in vital signs and mental status

107

Phenelzine

Non-selective MAO inhibitor

108

Serotonin synthesis

Tryptophan, 5-hydroxytryptophan, 5-hydroxytriptamine

109

Buspirone

5-HT1A partial agonist
antidepressant (non BZD)

110

Venlafaxine, Duloxetine

SNRIs

111

Side effects or problems with tricyclic antidepressants

Coma, convulsions, confusion in elderly, cardiotoxicity

112

LSD

non-selective serotonin agonist
Binds to all serotonin receptors except 5-HT3 and 5-HT4

113

selegiline

MAO-B inh

114

Monoamine hypothesis of depression

Depression results from a decrease in serotonin and norepinephrine transmission

115

Nortriptyline

TCA

116

Modafanil, armodafanil

amphetamine
-depression

117

dexmethylphenidate, methylphenidate

amphetamine
-depression

118

lisdexamphetamine

amphetamine
-depression

119

isocarboxazil, phenelzine

nonselective MAOI
-depression

120

tranylcypromine

MAOI
depression

121

Amitriptyline

TCA
-sedating can use for insomnia

122

clomipramine

TCA

123

Desipramine

TCA

124

Doxapin

TCA
-low dose used for insomnia though H1

125

Imipramine

TCA

126

citalopram, escitalopram

SSRI

127

fluvoxamine

SSRI

128

Milnacipram

SNRI

129

Trazodone

Atypical antidepressants
-sedating, can use for insomnia

130

Mirtazapine

Atypical antidepressant
-sedating, can use for insomnia

131

BDZ and hepatic induction

Benzodiazepines do not induce hepatic microsomal enzymes

132

CBT

Often used in conjunction with SSRIs for anxiety

133

BZD adverse effects

Sedation, tolerance, physical dependence, self-administration

134

Clonazepam uses

Panic, anxiety, seizure

135

PTSD first line treatment

SSRI, usually paroxetine or sertraline

136

Flumazenil

BZD antagonist

137

BZD toxicity

Impaired judgement, slurred speech, incoordination, stupor, respiratory depression, death

138

Barbiturates

Bind to a distinct subunit combination on the GABA receptor and at high concentrations can open the channel on their own (without GABA).

139

Sedating antidepressants

Trazodone, mirtazapine, amyitriptyline

140

Which drugs are typically used for sleep?

Eszoiclone, hydroxyzine, zolpidem, zaleplon, ramelteon

141

GABA binding site on GABA R

alpha-1 and beta-2 subunits

142

Non-BZD GABA A agonists

Eszopiclone, zolpidem, zaleplon
(hypnotics)

143

Doxepin

Tricyclic antidepressant, low dose mechanism for insomnia is histamine H1

144

GABA shunt

Refers to alpha ketoglutarate from the Krebs Cycle, converted to glutamic acid by GABA-transaminase; then subsequently to GABA by glutamic acid decarboxylase (GAD). GABA is then metabolized to form succinic semialdehyde to succinic acid and returns to the Krebs Cycle.

145

Alprazolam uses

panic, anxiety
(short acting)

146

Diazepam uses

Anxiety, insomnia, pre-op, muscle relaxant, status epilepticus

147

Flurazepam, Temazepam and Triazolam use

insomnia
(BZDs)

148

Nonbenzodiazepine anxiolytic

Buspirone mechanism is serotoniergic 5-HT1A receptor partial agonist

149

General anxiety disorder first line treatment

SSRI, usually venlafaxine, paroxetine or escitalopram

150

Insomnia disorder

Insomnia complaint and significant daytime impairment

151

Glutamine loop

Glutamine is formed as GABA is transaminated and converted to glutamine. The glutamine is reconverted to glutamate; then decarboxylated by neuronal GAD to GABA

152

Zolpidem disadvantages

(Non BDZ GABA agonist)
4-6 hr effect, therefore not for middle of the night awakenings, associated with parasomnias

153

BZD binding site on GABA A R

gamma-2 and alpha-1 subunits.

154

Short acting BZDs

Alprazolam, triazolam, lorazepam, oxazepam

155

Lorazepam uses

anxiety, alcohol related seizure, status epilepticis

156

BDZ used for sleep

Estazolam, flurazepam, quazepam, temazepam, triazolam

157

Long acting BZDs

Flurazepam, clorazepate, prazepam

158

Traditional BZD disadvantages

Rebound insomnia, memory impairments, loss of coordination, abuse potential, not good for those with respiratory conditions

159

Chlordiazepoxide use

alcohol detox

160

Zolpidem advantages

Shorten sleep latency, improve duration, can be used as needed, no negative effect on sleep architecture

161

Antipsychotics with CV effects

Chlorpromazine, Thioridazine, Ziprazidone, Asenapine

162

Butyrophenones are:

Haloperidol, Droperidol
(typicals)

163

All atypical antipsychotics:

D2 receptor antagonists and block 5-HT2

164

Clozapine

Azepine atypical antipsychotic
-Associated with 1% risk of agranulocytosis, myocarditis

165

Antipsychotic with the longest half-life:

Aripiprazole

166

Classes of typical antipsychotics:

Phenothiazines, Thioxanthenes, and Butryophenones

167

Patients taking clozapine must be monitored for

Agranulocytosis

168

The phenothiazine class is:

typical antipsychotic (block D2)

169

Antipsychotics and the tuberoinfundibular pathway

Typical antipsychotics blocking this dopaminergic pathway lead to prolactin secretion

170

Aripiprazole

-Atypical antipsychotic, longest half life, in top 25 prescribed drugs
Is especially helpful for negative symptoms; is more activating than sedating

171

Pos schizo symptoms

Delusions, hallucinations, thought disorder, aggressive behaviors, stereotyped movements

172

Dopamine released from the hypothalamus blocks ______ via _______

prolactin via the tuberoinfundibular pathway

173

Tardive dyskinesia

Develops after months or years, seen in 20-40% of patients on typical antipsychotics, often irreversible; consists of involuntary movements often of the face and tongue, trunk and limbs - severely disabling often

174

Sedation with antipsychotics is caused likely by:

Histamine H1 receptor involvement

175

Quetiapine

-atypical azepine antipsychotic
Known for association with lens changes; requires an eye examination at initiation and at 6-month intervals

176

Mesolimbic tract

Ventral tegmentum to limbic area. First generation antipsychotics block D2 receptors, theory that this tract was involved.

177

Serotonin theory of schizophrenia

Direct and indirect 5-HT agonists exacerbate the symptoms of schizophrenia

178

Serotonin hyperactivity is assoc with:

Positive and negative symptoms of schizophrenia; second generation antispychotics (atypicals) block 5HT2 receptors in addition to D2 receptors

179

Extrapyramidal motor disturbances (EPS):

-Antipsychotics
Are reversible, involve involuntary movements, occur in the first few weeks and diminish with time; are less with atypical drugs

180

Glutamate theory of schizo

Observations that PCP induces acute psychotic, schizophrenia like symptoms

181

Major SEs of typical antipsychotics

Extrapyramidal symptoms (Parkinsonism, dystonias, akathesia; tardive dyskinesia

182

Mech of typical antipsychotics

D2 dopamine receptor antagonism

183

Typical anti-psychotics antagonist what to cause their effects?

Noradrenergic alpha-1, histamine H1 and muscarinic M1 receptors

184

Atypical antipsychotics got the name due to:

No or low extrapyramidal symptoms

185

Olanzapine

-Azepine atypical antipsychotic
-Weight gain

186

Therapeutic effects of antipsychotics req:

80% occupancy of dopamine D2 receptors based on imaging studies

187

Weight gain is seen with which types of antipsychotics?

Atypicals

188

Risperidone

-Atypical antipsychotic
Demonstrates hyperprolactinemia even at low doses

189

Sertindole

atypical antipsychotic

190

sulpiride

atypical antipsychotic

191

ziprasidone

atypical antipsychotic
-CV

192

Molindone

atypical antipsychotic

193

paliperidone

atypical antipsychotic

194

zotepine

atypical antipsychotic azepine

195

Lozapine

azepine atypical antipsychotic

196

thiothixine

typical antipsychotic thioxanthene

197

Zuclopentixol

typical antipsychotic thioxanthene

198

Flupenthixol

typical antipsychotic thioxanthene

199

Chlorprothixene

typical antipsychotic thioxanthene

200

Trifluoperazine

typical antipsychotic phenothiazine

201

Perphenazine

typical antipsychotic phenothiazine

202

Mesoridazine

typical antipsychotic phenothiazine

203

Thioridazine

typical antipsychotic phenothiazine
-low potency
-CV

204

Fluphenazine

typical antipsychotic phenothiazine

205

Chloralhydrate

barbiturate-like antidepressant

206

Eczopiclone

non BDZ hypnotic GABA A agonist

207

Zaleplon

non BDZ hypnotic GABA A agonist
-typically used for sleep

208

Flurazepam

long acting BZD hypnotic

209

Triazolam

short acting BZD hypnotic used for sleep

210

Halothane

inhale anesthetic
-hepatitis

211

Thiopental

iv anes

212

Methohexital

iv anes

213

propofol

iv anes
-can be used as aole (no muscle relaxant)

214

ketamine

iv anes
-dysphoria, low dose analgesia, CV stimulant
*exception incr cerebral bl fl

215

Fentanyl

iv anes
-analgesia

216

novocaine

first inject LA (ester)
-metab in plasma

217

tetracaine

LA (ester)
incr pka so slow onset, long duration
-topical

218

2-chloropricaine

LA (ester)

219

Benzocaine

first synthetic LA (ester)
-methemoglobinemia, low pka nonionized base

220

Lidocaine

amide LA prototype

221

mepivacaine

amide LA
similar to lidocaine but less vasodilation
-accumulation don't use for long epidural

222

Dibucaine

LA topical cream (amide)

223

Bupivacaine

LA (amide)
-long acting
-cardiotoxic (fix with intralipid)
-Freq dependent block
-spinal

224

Ropivacaine

LA AMide
-compare to Bupivavaine, lower cardiotox, lower potency, beter freq dependent block, long lasting but not as long.

225

Prilocaine

-LA amide
-methemoglobinemia
-most rapid metab

226

Nitrous Oxide

anesthetic with highest MAC

227

BZD and anesthesia

Sedatives only, not anesthetics; no analgesia; effects partially antagonized by flumazenil

228

Opoids and anesthetics

Analgesics not anesthetics; can reduce the amount of anesthetic required; effects 100% reversible with naloxone

229

Physical properties of LAs

Weak bases, poorly water soluble; synthetics derived from cocaine

230

Unmyelinated nerve fibers and LA

Small (B and C) fibers appear more sensitive to local anesthetics

231

Duration of action anesth

Directly proportional to protein binding; also relates to toxicity - high protein binding reduces amount of free drug

232

Long acting LAs

Bupivacaine and Ropivacaine

233

LA toxicity initial signs

Central nervous system: lightheadedness, peri-oral numbness, dizziness, visual and auditory disturbances, disorientation, drowsiness.

234

LA peripheral toxic signs

Vasoconstriction (low doses); vasodilation (high doses); chest pain, shortness of breath, palpitations,
more

235

Sufentanil

-more potent than fentanyl
-ultra short acting
-respiratory depression

236

Narcotic

Any psychoactive compound with sleep-inducing properties. Today means totally prohibited

237

Relatively selective COX II

Celecoxib, diclofenac

238

COX I selective drugs

Flurbiprofen
ketorolac

239

Butorphenol

Kappa opioid receptor agonist and mu opioid receptor antagonist or partial agonist

240

Non opoid Non NSAID drugs

Acetaminophen, Tramadol

241

Heroin

Rapidly metabolized to morphine. Due to rapid brain penetration, heroin causes an intense euphoria. Not used clinically in U.S.

242

Acetaminophen

Non opoid non NSAID
-Does not produce GI damage, ineffective in intense pain, narrow therapeutic index - liver damage

243

Oxycodone

Semisynthetic weak opioid agonist used in combination with NSAIDs for analgesia.

244

Non-selective COX inhs

Ketoprofen, aspirin, naproxen, ibuprofen, indomethacin, sulindac

245

SE aspirin

GI upset; hypersensitivity-like reaction; Reye's syndrome; anticoagulant

246

Opoid agonist prototype

morphine

247

Naloxone

NARCAN; pure opioid antagonist, most potent at the mu receptor

248

COX 1

Constitutively active enzyme, involved in GI protection, platelet function, regulation of blood flow and kidney function

249

Codeine

Weak mu opioid agonist used as antitussive and analgesic in mild pain. Prodrug for morphine

250

COX II

Inducible enzyme, involved in inflammation, pain, fever and cardiovascular function

251

Celecoxib

Osteoarthritis and rheumatoid arthritis in adult patients, acute pain an dysmenorrhea; increased risk of major cardiovascular problems (30%)

252

Loperimide

IMODIUM, a mu opioid agonist that is poorly absorbed after oral administration; used as an antidiarrheal. Does not cross the blood brain barrier

253

Mechanism of NSAID renal effects

Inhibit prostaglandin synthesis allowing vasoconstriction leading to acute renal failure

254

Meperidine

Synthetic, weak mu opioid agonist used for analgesia during delivery.

255

Methedone

Orally active long acting mu opioid receptor agonist. Does not cause significant euphoria. Cross tolerance with morphine or heroin and therefore useful with addicts

256

Surgical treatment for chronic pain

Cut spinothalamic tract

257

Morphine SEs

Euphoria, sedation, respiratory depression, nausea and vomiting, constipation, reduced release of hormones (GnRH and CRF) from hypothalamus

258

A-delta fibers

Lightly myelinated axons, rapid condution of signal, mediate the fast, pricking or sharp quality of pain

259

Nigro-striatal dopaminergic pathway

substantia niagra to striatum

260

VTA

dopiminergic cell bodies

261

Raphae nucleus

serotonin cell bodies

262

Tuberoinfundibular pathway

Hypothalamus to anterior pituitary

263

Nucleus basalis

Acetylcholine neuronal cell bodies

264

Locus cereuleous

NE cell bodies

265

PCP can produce

hallucinations (incr glut)

266

Drugs of abuse produce their effects through:

Through G-protein coupled receptors, ionotropic receptors and monoamine transporters

267

The mesolimbic pathway including the nucleus accumbens

Is responsible for the mood elevating euphoria and rewarding effects of cocaine and amphetamine

268

Hallucinogens

Increase extracellular glutamate in the prefrontal cortex through stimulation of postsynaptic 5-HT2A receptors

269

Varenicline

Partial agonist of nicotinic acetylcholine receptors used for smoking cessation

270

Acamprosate

Antagonist of NMDA receptor used for treatment of alcoholism

271

Types of tolerance

Pharmacokinetic, pharmacodynamics, behavioral, and inverse (sensitization)

272

Anandamide

endogenous ligand for cannabinoids

273

PCP mech of action

Noncompetitive NMDA calcium channel blocker

274

Alcohol mech of action

Blocks NMDA receptor and enhances GABA receptor (through GABA-A)