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Pharm 2 > Test 1 Material > Flashcards

Test 1 Material Flashcards

0
Q

Types of Anxiety Disorders

A
  • Generalized Anxiety Disorder
  • Specific phobias
  • Social phobia
  • Panic disorder (+/- agoraphobia: fear of open spaces)
  • OCD
  • PTSD
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1
Q

Anxiety

A
  • Tension, unease, apprehension
  • Symptoms of fear include tachycardia, sweating, trembling, palpitations (common complaints include chest pain and nausea)
  • one of the most commonly seen complaints
  • Overreaction to unknown source or real stimulus
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2
Q

Benzodiazepines

MOA

A
  • are inhibitory via GABA (gamma amino butyric acid) receptor (linked to chloride ion channel; causes Cl- influx=hyperpolarization, thus decreasing neuronal firing)
  • bind to allosteric site (increase affinity of GABA for receptor)
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3
Q

Benzodiazepines

Actions

A
  • anxiolytic (all, low doses), sedation/hypnotic (all, high doses), anterograde amnesia, anticonvulsant activity (some), muscle relaxation
  • all LACK autonomic side effects, antipsychotic actions, analgesic actions
  • high therapeutic index (relatively safe)
  • Dependence can develop: psychological and physical, withdrawal can cause confusion, anxiety, agitation, and insomnia
  • Side effects are drowsiness, confusion, ataxia, and cognitive impairment
  • Caution in patients with liver disease, narrow angle glaucoma, alcohol and other CNS depressants; be aware or rebound anxiety, avoid in patients with history of substance abuse
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4
Q

Benzodiazepines

DOA

A
  • Short Acting (oxazepam, triazolam, midazolam)
  • Intermediate (alprazolam, temazepam, lorazepam)
  • Long Acting (diazepam, flurazepam, clonazepam, chlordiazepoxide, clorazepate)
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5
Q

Benzodiazepines

Therapeutic uses

A
  • Anxiety disorders (severe: diazepam (DOC); for infrequent events: short acting like triazolam; sometimes beta blockers can be helpful; for refractory cases: SSRI)
  • Panic Attacks: alprazolam
  • Amnesia: midazolam
  • Muscle relaxation: diazepam
  • Seizures: clonazepam (chronic epilepsy); diazepam (grand-mal seizures)
  • Alcohol withdrawal: chlordiazepoxide, clorazepate, diazepam, lorazepam, oxazepam
  • Sleep Disorders: flurazepam (daytime sedation), temazepam (for frequent awakening), triazolam (for problems going to sleep, tolerance develops quickly); all decrease sleep induction time and number of awakenings and decrease sleep duration
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6
Q

Flumazenil

A

-Benzodiazepine antagonist
Used for rapid reversal of sedation and or overdose; IV only, rapid onset, short duration
-Adverse: BZ withdrawal, seizures, dizziness, N/V, agitation

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7
Q

Other anxiolytic drugs

Besides benzodiazepines

A

Buspirone (BuSpar)
Hydroxyzine
Antidepressants

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8
Q

Buspirone (BuSpar)

A
  • For GAD (constant, at least 6months), stimulates serotonin 5-HT 1A receptors (as well as DA2 and 5-HT 2A); no anticonvulsant or muscle relaxation, minimal sedation, cognitive dysfunction and dependence
  • adverse effects: headache, dizziness, nervousness, slow onset of action
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9
Q

Hydroxyzine

A
  • Antihistamine and antiemetic
  • Sedation is main action
  • little habituation; used when history of drug dependence
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10
Q

Antidepressants

A
  • Proven efficacious in some patients with chronic anxiety disorders
  • First line when concerned about addiction/dependence
  • SSRIs, TCAs, venlafaxine, duloxetine, MAOIs
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11
Q

Other sedative/hypnotic agents

Besides benzodiazepines

A
  • eszopiclone (lunesta)
  • ramelteon
  • zaleplon
  • zolpidem (ambien)
  • chloral hydrate
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12
Q

Eszopiclone (lunesta)

A

Acts on subset of BZ1 sites on GABA receptors, no anticonvulsant or muscle relaxation, withdrawal or tolerance develop with long term use, rapid onset and elimination, oral sedative, effective up to 6 months
-adverse effects: anxiety, dry mouth, chest pain, headache, migraine, edema, unpleasant taste

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13
Q

Zolpidem (Ambien)

A

Acts on subset of BZ1 sites on GABA receptors, no anticonvulsant or muscle relaxation, no withdrawal or tolerance, rapid onset and elimination, requires CYP3A4 for metabolism
-Adverse effects: nightmares, agitation, headache, GI upset, dizziness, daytime drowsiness

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14
Q

Zaleplon (Sonata)

A

Acts on subset of BZ1 sites on GABA receptors, no anticonvulsant or muscle relaxation, no withdrawal or tolerance, rapid onset and elimination, requires CYP3A4 for metabolism
-Adverse effects: nightmares, agitation, headache, GI upset, dizziness, daytime drowsiness

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15
Q

Ramelteon (rozeram)

A
  • Melatonin MT1 and MT2 receptor agonist (these are associated with maintenance of circadian sleep rhythm through the inhibitory activity on excitatory wakefulness promoting circuits in the suprachiasmic nucleus
  • Adverse effects: headache, somnolence, fatigue, dizziness, nausea, insomnia, respiratory infection
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16
Q

Barbiturates

MOA

A
  • Have been replaced by benzodiazepines for sedation, induction and maintenance of sleep
  • MOA: increase GABA action of Cl through non BZ sites, block glutamate receptors and Na channels, decrease mesencephalic reticular activating system
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17
Q

Barbiturates

Actions

A
  • CNS depression: sedation, hypnosis, anesthesia
  • NO ANALGESIA!!!
  • respiratory depression - coma - death
  • induces CYT P450
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18
Q

Barbiturates

Therapeutic uses

A

Anesthesia (thiopental)
Anticonvulsant (phenobarbital)
Anti anxiety ???

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19
Q

Barbiturates

Adverse effects

A

-impair concentration, drug hangover/addiction potential, P450 effects, CI in acute intermittent porphyria (expose/exaggerate disease by inducing heme synthesis), OD potential

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20
Q

Stimulants

-General categories

A
  • Psychomotor: methyxanthines (caffeine, theophylline), nicotine, cocaine, amphetamine, methylphenidate
  • Psychotomimetics: LSD (lysergic acid diethylamide), tetrahydrocannabinol, PCP (phencyclidine)
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21
Q

Psychomotor Stimulants

A

Excitement, euphoria, decreased fatigue, increased motor activity
-few clinical uses but important drugs of abuse

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22
Q

Methylxanthines

Caffeine and Theophylline

A

Psychomotor Stimulants

  • MOA: phosphodiesterase inhibitors (increase cAMP, cGMP), adenosine receptor antagonists
  • Actions: decrease fatigue, increase mental alertness, increase chronotropic and inotropic effects, diuretic action, increases HCl acid production
  • therapeutic uses: relaxes smooth muscles in bronchioles
  • adverse effects: can cross placenta and is excreted in breast milk, insomnia, anxiety, agitation, high dose toxicity (emesis, tremors, convulsions)
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23
Q

Nicotine

A

Psychomotor Stimulant

  • one of the most addicting substances known
  • CNS and Ganglionic stimulation (high dose-blockade)
  • actions: euphoria, arousal, relaxation, increases attention, central respiratory paralysis, severe hypotension (last 2 @ high doses); increase BP and HR, decrease coronary blood flow, motor activity of bowel
  • Adverse: irritability and tremors, intestinal cramping and diarrhea, increases metabolism of many drugs, withdrawal/physical dependence (anxiety, agitation, headache, insomnia
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24
Q

Smoking cessation

A
  • Nicotine Patch
  • Bupropion SR: antidepressant, dopamine and NE reuptake inhibitor
  • Varenicline (Chantix): most effective drug available; nicotinic receptor partial agonist (more potent, less efficacious than nicotine, results in dopamine release)
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25
Q

Cocaine

A
  • MOA: blockade of NE, serotonin and dopamine reuptake (prolongs dopaminergic effects in the brain causing euphoria)
  • Actions: increases mental awareness and euphoria, can cause hallucinations, delusions and paranoia, high doses can produce tremors, convulsions, respiratory and vasomotor depression, SAS (tachycardia, HT, pupillary dilation, peripheral vasoconstriction, necrosis of nasal septum)
  • therapeutic uses: local anesthetic (ophthalmic, ENT) (only anesthetic with intrinsic vasoconstriction activity)
  • Adverse effects: anxiety (HT, tachycardia, sweating, paranoia), depression, cardiac arrhythmias, seizures, incidence of MI unrelated to dose/duration/route
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26
Q

Amphetamines

A

Psychomotor Stimulants

  • effects similar to cocaine
  • MOA: releases intracellular stores of catecholamines and blocks MAO
  • Actions: stimulates cerebrospinal axis, cortex, brain stem, medulla (increases alertness, decreases fatigue, appetite and insomnia), high dose (convulsions), SAS (stimulated indirectly)
  • Therapeutic uses: ADD, narcolepsy (amphetamine (Adderal), methylphenidate (Ritalin); both are schedule II)
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27
Q

Amphetamine

Adverse effects

A
  • CNS: confusion, insomnia, irritability, weakness, vertigo, dizziness, tremor, hyperactive reflexes, delirium, panic, suicide, amphetamine psychosis
  • CVS: palpitations, arrhythmias, HT, angina, circulatory collapse, headache, chills, sweating
  • GI: anorexia, N/V and D, abdominal cramping
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28
Q

Psychotomimetics

Hallucinogens

A
  • primary action is to induce altered perceptual states

- incapable of normal decision making

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29
Q

LSD

A

Psychotomimetic

  • acts as serotonin agonist
  • Actions: activation of SAS (pupillary dilation, inc BP, temp and piloerection), low dose (hallucinations and mood alteration) high dose (long lasting psychotic changes)
  • adverse effects: hyperreflexia, nausea, weakness
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30
Q

Tetrahydrocannabinol (dronabinol)

A
  • Use: antiemetic in cancer chemo
  • Adverse: inc HR, dec BP, conjunctival reddening, toxic psychosis
  • Actions: euphoria, relaxation, drowsiness, impairs short term memories, dec strength, impairs highly skilled motor activity, inc appetite, visual hallucinations, sensory enhancement, delusions
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31
Q

PCP

A

-MOA: inhibits reuptake of dopamine, serotonin 5-HT and NE; dissociative anesthesia and numbness of extremities, staggered gate, slurred speech, muscular rigidity, hostile/bizarre behavior, higher dose (anesthesia, stupor or coma, inc sensitivity to external stimuli), CNS actions may persist for a week, anticholinergic but hyper salivation

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32
Q

Depression types

A
  • Reactive Depression (60%, secondary): occurs in response to grief, illness, loss; treatment includes psychotherapy or acute therapeutics
  • Major Depression (25%, endogenous): genetic, inability to experience ordinary pleasure or cope with daily life; treated with antidepressants or ECT
  • Bipolar disorders (10-15%, manic-depressive): characterized by cyclic periods of mania; treated with lithium in combination with antidepressants and/or antipsychotic agents
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33
Q

Mood altering illnesses

A
  • depression: feelings of sadness, hopelessness, despair, inability to experience pleasure in daily activities; biogenic amine theory (depression is due to a deficiency of NE and serotonin in key sites in the brain)
  • mania: enthusiasm, rapid thought and speech, extreme self-confidence, and impaired judgement; biogenic amine theory (mania is caused by an overproduction of NE, dopamine, and serotonin)
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34
Q

Symptoms of depression

A

Loss of interest (anhedonia), sleep disturbance, appetite change, depressed mood (dysthymia), concentration problems, activity diminished, guilt, energy diminished, suicidal ideation

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35
Q

Manic symptoms

A

Thought to be due to nt over activity
Inflated self esteem, grandiosity, irritability, pressured speech, distractibility, impaired judgement, psychomotor agitation

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36
Q

Non-drug Therapy for Depression

A 
Psychotherapy (best results when combined with drugs)
Electroconvulsive Therapy (recommended for treatment resistant, vegetative, and psychotic depression)
37
Q

Classes of drugs to treat depression

A

TCAs, SSRIs, SNRIs, atypical antidepressants, MAOIs, antimanics (lithium, anticonvulsants)

All potentiate, either directly or indirectly, NE and 5-HT, all equally effective about 50-70%

38
Q

TCAs

Drugs and MOA

A

1st gen: Amitriptyline, Desipramine, Doxepin, Imipramine, Nortriptyline
2nd gen: Amoxapine, Maprotiline
3rd gen: SSRIs (??)
MOA: block the reuptake of NE and serotonin into presynaptic terminals, block alpha adrenergic, histamine and muscarinic receptors

39
Q

TCAs

Actions and therapeutic uses

A

Elevate mood, improve mental alertness, increase physical activity, reduce morbid preoccupation
-therapeutics: moderate to severe depression, some panic disorders, bed wetting (imipramine)

40
Q

TCAs

Side effects

A
  • weight gain, antihistamine (sedation), anticholinergic (dry mouth, urinary retention, constipation, blurred vision, glaucoma), alpha antagonist (OH, reflex tachycardia), cardiovascular (fatal arrhythmias)
  • narrow therapeutic index (careful with manis-depressive and suicidal)
  • interaction with ethanol and other CNS depressants: toxic depression
41
Q

SSRIs

Drugs and MOA

A

Citalopram (Celexa), Escitalopram (Leaxpro), Fluoxetine (Prozac), Fluvoxamine (Luvox), Paroxetine (Paxil), Sertraline (Zoloft)

MOA: selective inhibition of serotonin reuptake (fewer anticholinergic effects, less cardio toxicity, less weight gain, no OH, can take 2-4 weeks to see effect, potent inhibitors of P450

42
Q

SSRIs

Therapeutic uses

A

Major depression, OCD (Fluvoxamine), bulimia/anorexia nervosa, panic disorder, PMS, post menopausal syndrome (hot flashes) (fluoxetine), GAD (?)

43
Q

SSRIs

Adverse effects

A

Nausea, sleep disturbances, insomnia (fluoxetine), sexual dysfunction (loss of libido, anorgasmia, delayed ejaculation), GI, anorexia, weight loss, suicidal ideation in children/teens, serotonin symptom (hyperthermia, rigidity), hallucinations
-prolonged QT interval (Citalopram, Escitalopram) which could lead to ventricular arrhythmia and death, other don’t show this

44
Q

SNRIs

A

Venlafaxine (Effexor), Desvenlafaxine (Pristiq), Duloxetine (Cymbalta)

  • safer than TCAs in OD, can be used when SSRIs have failed
  • especially used for depression associated with neuropathic pain
  • no adrenergic, muscarinic, histaminergic receptor blockade (few adverse effects: nausea, headache, dry mouth, somnolence, sexual dysfunction)
45
Q

Atypical antidepressants

Drugs

A

Bupropion (Wellbutrin), Mirtazapine (Remeron), Trazadone, Nefazodone

46
Q

Bupropion (Wellbutrin)

A

Atypical Antidepressant; Weak NE/DA reuptake inhibitor, no anticholinergic, antihistamine, or alpha blockade

  • low incidence of sexual dysfunction, has been used for smoking cessation
  • Adverse effects: xerostomia, sweating, nervousness, tremor, lowers seizure threshold (CI in patients with previous seizure disorders)
47
Q

Mirtazapine (Remeron)

A

Atypical antidepressant, alpha 2 antagonist- increases 5HT and NE neurotransmission; 5HT2 serotonin antagonist; antihistamine (H1-sedation)
-increase appetite, weight gain, no anticholinergic, little sexual dysfunction, minimal drug interactions

48
Q

Trazadone and Nefazodone

A

Atypical Antidepressants, 5HT2A antagonists, weak 5HT reuptake inhibitors, desensitizes 5HT1A Presynaptic receptors (inc 5HT release)

  • antihistamine (H1-sedation); low incidence of sexual dysfunction (Trazadone-priapism), fewer anticholinergic side effects than TCAs
  • Nefazodone: hepatotoxicity
49
Q

MAOIs

Drugs and MOA

A

Phenelzine, Tranylcypromine, Isocarboxazid, Selegiline

  • MOA: inhibit mono amine oxidase, inc stores of intraneuronal NE, DA, and serotonin
  • Food-drug interactions (tyramine: hypertensive crisis - HT, tachycardia, nausea, arrhythmias, stroke
50
Q

MAOIs

Uses and adverse effects

A
  • only used in patients refractory or hypersensitive to other antidepressants; strong anxiety, phobic states, atypical depression (labile mood, rejection sensitivity, appetite disorders)
  • AE: tyramine, drowsiness, OH, blurred vision, xerostomia, constipation, urinary retention, do not use with SSRIs (serotonin syndrome)
51
Q

Serotonin syndrome

A

Potentially fatal interaction caused by the combination of two or more drugs http enhance serotonin transmission

  • symptoms: anxiety, shivering, tremor, diaphoresis, death due to malignant hyperthermia
  • most cases from MAOIs and SSRIs, but others include meperidine, TCAs, dextromethorphan, lithium, triptans
52
Q

Bipolar disorder

A
  • considered the most deadly psychiatric illness due to suicide rate
  • manic (impair function) and hypomanic episodes are both characterized by a distinct period of abnormally and persistently elevated, expansive or irritable mood
53
Q

Lithium Salts

A

Used in the treatment of manic-depressive illnesses (not used for acute mania due to 1-2 week delayed drug effect)
Unknown MOA
Toxic drug with narrow TI
Drug interactions: NSAIDs will increase levels

54
Q

New Bipolar treatment

A
  • olanzapine + fluoxetine
  • atypical + SSRI
  • manic disorders + depression
  • anticonvulsants: mood stabilizers (carbamazepine, valproic acid/depakote, lamotrigine/lamictal)
55
Q

Psychotic Disorders

General

A
  • positive symptoms: delusions, hallucinations, disorganized speech, bizarre behaviors
  • negative symptoms: neurovegetative, flat affect, poor eye contact, lack of goal directed activity
  • most patients exhibit both types, thought to be DA or serotonin
56
Q

Neuroleptic drugs

Antipsychotic, antischizophrenia, major tranquilizers

A

Older drugs MOA: competitive blockers of D2
Newer drugs MOA: “atypical”, block serotonin 5HT2
-also block M, alpha, H receptors to varying degree
-do not cure, but permit function
-all have equivalent therapeutic efficacies

57
Q

Antipsychotic actions

A
  • all reduce the positive symptoms (hallucinations, agitation) by blocking dopamine receptors
  • the antipsychotic effects take several weeks to be effective
  • calming effect, reduce spontaneous physical movement
  • 1st gen are most effective against “positive” symptoms, newer atypical agents are effective in “negative” symptoms
  • anticholinergic: helps minimize the risk of extra pyramidal symptoms (EPS) with 1st gen
  • antiemetic: due to blockage of D2 in the CTZ of the medulla, 2nd gen less effective
  • tranquilizers: used to handle agitated and disruptive behavior
  • pain control (need opioid), intractable hiccups (chlorpromazine)
58
Q

Antipsychotic

Adverse effects

A
  • to D2 blockade: akathesia (restlessness), EPS, tardive dyskinesia (inability to control facial movements, Barty Crouch jr.), gynecomastia, amenorrhea, galactorrhea, typical ones show more than atypical
  • anticholinergic: xerostomia, urinary retention, constipation, loss of accomodation
  • neuroleptic malignant syndrome: rare and potentially fatal, high fever, autonomic instability, muscle rigidity
  • anti adrenergic: OH
59
Q

Antipsychotics

Cautions/warnings

A
  • May cause drowsiness, avoid with alcohol and other depressants, CI in glaucoma and prostatic hypertrophy, caution in CV and hepatic disease, safety in pregnancy has not been established
  • FDA must put info on hyperglycemia and diabetes on all atypical ones
60
Q

Chlorpromazine

A

1st gen low potency antipsychotic

-used to control manifestations of mania, intractable hiccups, highest occurrence of sedation

61
Q

Fluphenazine

A

1st gen high potency antipsychotic

-good in patients refusing oral meds because it comes in depot injection, also as IM and decanoate

62
Q

Haloperidol

A

1st gen high potency antipsychotic

  • common EPS due to low anticholinergic action, used for acute agitation, available as po, IM, decanoate
  • used for acute manifestations of mania, control of agitation
  • rapid acting, causes less drowsiness than the rest of the antipsychotics
63
Q

Clozapine

A

2nd gen atypical antipsychotic
-excellent for negative symptoms, low risk for EPS or tardive dyskinesia, high risk for agranulocytosis, reserve for refractory pts

64
Q

Risperidone

A

2nd gen atypical antipsychotic

  • less toxicity than haldol, no agranulocytosis risk, 1st line therapy
  • adverse: OH, reflex tachycardia
  • fewer risks with EPS and TD
65
Q

Newer atypicals

A

2nd gen atypical antipsychotic

  • Zyprexa: weight gain and diabetes can occur
  • Seroquel: less weight gain
  • Geodon: no weight gain, QT prolongation (?)
  • all: low risk for EPS and TD with no agranulocytosis risk
66
Q

Phenothiazine for N/V

A

Avoid in children and trivial N/V, can cause EPS and other adverse effects
-also prochlorperazine, promethazine, droperidol, trimethobenzamide

67
Q

Types of pain

A
  • nicoceptive: travels through functional nervous system reporting potential or actual tissue injury
  • neuropathic: through dysfunctional nervous system reporting injury to nervous system (peripheral neuropathy)
  • acute: short, well characterized, known cause
  • chronic: outlives normal healing period
68
Q

Opioid terminology and MOA

A
  • Opioid: natural and synthetic substances that produce morphine type effects
  • opiate is a term reserved for natural substances from the opium poppy
  • opioids bind to opioid receptors in the CNS to mimic endogenous nts (endorphins, enkephalins); they hyper polarize membranes thus inhibiting depolarization (dec cAMP and Ca influx and inc K efflux
  • primary use is to relieve pain and the anxiety that accompanies pain
69
Q

Opioids to remember

A
  • strong agonists: Morphine, Meperidine, Methadone, Fentanyl, Heroin, Hydromorphone, Hydrocodone, Oxycodone, Oxymorphine
  • moderate agonists: Codeine, Propoxyphene (gone)
  • mixed agonist-antagonists (stimulates some receptors and block others; no recent exposure = analgesia; recent exposure = acute withdrawal; can develop dependence): Pentazocine, Buprenorphine, Butorphanol, Nalbuphine
  • opioid antagonists (no analgesia; chronic use: acute withdrawal, naive patients: no problem; used to reverse coma or respiratory depression of opioid OD, May not help, but usually doesn’t hurt): Naloxene, Naltrexone
70
Q

Opioid receptors

A
  • mu: supra spinal analgesia, respiratory depression, euphoria, sedation, physical dependence, dec GI motility, miosis
  • delta: analgesia, peripheral enkephalin
  • kappa: spinal analgesia, sedation, dysphoria, miosis
  • sigma: dysphoria, hallucinations, psychotomimetic effects, mydriasis
71
Q

Morphine (MOA)

A
  • binds with opioid receptors in CNS and GI track, causing hyperpolarization of nerve cells
  • prototype of opioid drugs
  • acts at mu most
72
Q

Morphine (actions)

A

Analgesia (raises pain threshold and alters the brain’s perception of pain w/o loss of consciousness), euphoria (pleasant floating sensation and freedom from anxiety and distress), anti-diarrheal (constipation, emetic, CTZ), cough suppression (antitussive), respiratory depression (dec CO2 response), treatment of acute pulmonary edema, miosis (no tolerance with time), histamine release (bronchoconstriction)

73
Q

Morphine (adverse reactions)

A

-severe respiratory depression, vomiting, dysphoria, allergy enhanced hypotensive effects, bronchospasm, inc intracranial pressure (ICP, enhanced cerebral and spinal ischemia), constipation, biliary tract (opioids constrict the sphincter of Oddi, inc biliary pressure- painful!), caution in BPH (urinary retention)

74
Q

Morphine (Cautions)

A

Neonates don’t conjugate=no morphine!!

Analgesic tolerance develops faster than respiratory depression, severe withdrawal

75
Q

Meperidine

A
  • synthetic opioid
  • causes respiratory depression, inc ICP, constipation, mydriasis, watch for hypotension postop, caution in dialysis pts (seizures)
  • used for analgesia, extensive use in labor
76
Q

Methadone

A
  • synthetic opioid
  • less euphoria, used for withdrawal from opioid addiction
  • causes analgesia, constipation, miosis, inc IPC, respiratory depression
77
Q

Fentanyl

A
  • Synthetic opioid
  • analgesia 80 times more than morphine, good for peri operative analgesia
  • transmucosal lollipop for children preop, patch for long duration
  • sufentanil: more potent than fentanyl
78
Q

Heroin

A

-acetylated morphine, three times more potent, easily crosses BBB, greater euphoria, no medical uses in US

79
Q

Codeine

A
  • synthetic opioid

- analgesia, antitussive (requires less than analgesic dose, being replaced by dextromethorphan)

80
Q

Pentazocine, Buprenorphine, Butorphanol

Mixed agonist-antagonist opioids

A
  • Pentazocine: kappa agonist, mu/sigma antagonist, caution in angina patients
  • Buprenorphine: partial mu agonist, long duration
  • Butorphanol: kappa agonist, partial mu agonist; nasal spray, can be used in labor
81
Q

Naloxene

A
  • opioid antagonist

- rapid onset (30sec), short half life (many opioids have longer-frequent dosing needed)

82
Q

Naltrexone

A
  • opioid antagonist (similar to Naloxene)

- longer half life, utility in rehabilitation (alcohol-decreases craving)

83
Q

Opioid withdrawal

A

6-12 hours: drug seeking, restlessness, lacrimation, rhinorrhea, sweating and yawning
12-24 hours: irritability, tremor, dilated pupils, anorexia, piloerection
24-72 hours: weakness, depression, N/V, abdominal cramps, diarrhea, chills, flushes, tachycardia, HTN, dehydration
7-10 days: alternating restless sleep
-intense craving remains (psychological dependence)

84
Q

Epilepsy

A
  • characterized by recurrent seizures (disturbance in cerebral function due to abnormal paroxysmal neuronal discharge in the brain)
  • primary (no specific cause found, idiopathic epilepsy, usually lifelong treatment)
  • secondary (underlying precipitating factor such as tumor, trauma, drug therapy, alcohol withdrawal, stroke; can often be treated with no further need for anti epileptic treatment)
85
Q

Classification of seizures

A
  • Partial: affecting only one part of the brain
  • -Simple: consciousness is usually preserved
  • -Complex: consciousness is usually impaired
  • -Be aware that these can become secondarily generalized at times
  • Generalized seizures (involves both hemispheres, loss of consciousness )
  • -absence (petit mal): usually in childhood and often “grow out of them”, brief unconsciousness with frequent staring/eye blinking
  • -myoclonic: brief single or multiple muscle contractions
  • -tonic-clonic (grand mal): sudden unconsciousness with rigidity (tonic phase) followed by jerking of muscles (clonic phase) for varying periods; postictal period (confusion, exhaustion)
  • -status epilepticus: rapid, recurrent seizures (can be life threatening, string of tonic-clonic or one that doesn’t end)
  • -febrile: benign but scary tonic clonic convulsions in children
86
Q

Benzodiazepines

Treatment of epilepsy

A
  • MOA: potentiate GABA receptor stimulation; generally mild on side effects but have abuse potential; need long acting med for chronic control
  • Diazepam: DOC for status epilepticus
  • lorazepam: status epilepticus
  • clonazepam: myoclonic
  • clorazepate
87
Q

Carbamazepine

A
  • not a benzodiazepine, sodium channel blocker; used for all partial and tonic-clonic seizures, also used for trigeminal neuralgia
  • AE: stupor, drowsiness, vertigo, ataxia, N/V, blurred vision, hyponatremia, Stephen Johnson syndrome, aplastic anemia, agranulocytosis, toxicity can cause coma
  • check liver function test and CBC baseline periodically
  • CYP inducer
88
Q

Suicide warning

A

FDA is concerned that ALL of the anti epileptic drugs may increase potential for suicide

89
Q

Epilepsy in pregnancy

A
  • all women should be on folic acid prior to conception
  • Divalproex and Barbiturates should be avoided
  • phenytoin (benefits outweigh the risks?)

Pharm 2 (1 decks)

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