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I hate DRUGS!! > CNS pharmacology > Flashcards

CNS pharmacology Flashcards

1
Q

An increase of chloride conductance is the most important result of activation of

A

GABAA receptors

  • GABA is the most important inhibitory transmitter in the brain
  • glcyine is also improtant in the spinal cord
  • GABA(a) receptors causes hyperpolarization mediated by increased chloride conductance
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2
Q

Neurotransmitters may ________

A
  • Increase chloride conductance to cause hyperpoarization
  • Increase potassium conductance to cause inhibition
  • Increase sodium conductance to cause excitation
  • Inhibit calcium conductanct to reduce transmitter release
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3
Q

All of the listed NT change membrane excitability by decreasing K conductance except _______

A

Dopamine

  • A decrease in K conductance is associated with neuronal excitation
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4
Q

Shares the same potassium channel as the 5-HT1A receptor

A

GABA(B) receptor

  • they share the same K channel with a G protein involved in the coupling mechanism
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5
Q

CHemicals most likely to function as a neurotransmitter in hierarchical systems

A

Glutamate

  • Aspartate
  • small numerous inhibitory interneurons which use GABA or glycine as transmitters
  • Drugs that affect hierarchical systsems often have profound effects on the overall excitability of the CNS
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6
Q

Actiavtion of metabotropic receptors located presynaptically causes inhibition by decreasing the inward flux of

A

Calcium

  • This type of presynaptic inhibition occurs after activation of dopamine D2, norepinephrine a2, metabotropic glutamate, and mu opiod peptide receptors
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7
Q

This transmitter is mostly located in diffuse neuronal systems in the CNS, with cell boides particlary in the raphe nuclei. It appears to play amjor role in the expression of mood states, and many antidepressant drugs are thought to icnreases its functional activity

A

Serotonin

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8
Q

Criteria for neurotransmitters

A
  • Present in higher concentration in the synaptic area than in other areas
  • Released by electrical or chemical stimulation via calcium dependent mechanism
  • produce the same sort of postsynaptic response
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9
Q

One of the first NT receptors to be identified in the CNS is loacted on the renshaw cell in the spinal cord. Activation of this receptor results in excitation via an increase in cation (Na, K) conductance independently of G protein-coupled mechanisms. Which compounds likely to activate this receptor

A

Nicotine

  • This results in the release of glycine, which via interaction with its receptors on the motor neuron causes membrane hyperpolarization
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10
Q

This neurotransmitter, found in diffuse systems, can exert both excitatory and inhibitory actions. Multiple receptor subtypes and a transporterd have been identified, some of which are targets for drugs that are used in major depressive disorder and attention deficit hyperactivity disorder

A

Norepinephrine

  • cell bodies of noradrenergic neurons located in the pons and brain stem project to all levels of the CNS
  • Most of the subclasses of adrenoceptors that occur in peripheral tissues are present in the CNS
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11
Q

This drug is used in the management of insomnia and facilitates the inhibitory actions of GABA, but it lacks anticonvulsant or muscle relaxing properties and has minimal effect on REM sleep. Its action are antagonized by flumazenil

A

Eszopiclone

  • Eszopiclone, zalepton, and zolpidem are related hypnotics that throught structurally different from benzodiazepines, appear to have a similar mechanism of action.
  • Not used in seizures or in muscle spasticity states
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12
Q

true of Barbiturates

A
  • Alkalinization of the urine accelerates the elimination of phenobarbital
  • withdrawl symptoms from use of short acting babiburates (secobarbital) are more severe than phenobarbital
  • The dose response curve for BZ is flatter than for barbiturates
  • Induction of liver- drug metabolizing enzymes occurs with barbiturates and may lead to decreases in half life of other drugs
  • Flumazenil is an antagonist at BZ receptors and are used to reverse CNS depresssant effect
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13
Q

A 24 year old has developed nervous disposition. He is easily startled, worries about inconsequential matters and sometimes complains of stomach cramps. At night, he grinds his teet in his sleep. Diagnosed as suffering from GAS, he is prescribed with buspirone. The patient should be informed to anticipate

A

That the drug is likely to take a week or more to begin working

  • Buspirone is a selective anxiolytic
  • minimal effects on cognition or memory
  • not additive with ethanol in terms of CNS depression
  • Tolerance is minimal
  • no dependency liability
  • not effective in acute anxiety. slow onset of action
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14
Q

MEchanism of action of benzodiazepines

A

Increase frquency of opening of chloride ion channels coupled to GABA(a) receptors

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15
Q

An 82 year old woman, otherwise healthy for her age has difficulty sleeping. Triazolam is prescribed for her at one half of the conventional adult dose.

A

The patient may experience amnesia, especially if she also consumes alcohol

  • In elderly patients taking benzodiazepines
    • hypotension
    • prone to CNS depressant
    • Additive effects on CNS depression
      • antihistamines
    • rebound insomnia
    • alcohol enhances psychomotor depression and the amnestic effects of the BZ
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16
Q

Flumazenil will counteract the effect of _______

A

Benzodiazepines

  • Binds to the chloride channel macromolecular complex and competes with the benzodiazepines, eszoporclone, zalepton, and zolpidem
  • It does not reverse the effects of barbiturates and buspirone
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17
Q

A 40 year old woman with occasional acute attacks of intense anxiety with marked physical symptoms, including hyperventilation, tachycardia, adn sweating. If she is diagnosed as suffering from a panic disorder, the most appropriate drug to use is

A

Alprazolam

  • Alprazolam and clonazepam are the most effective of the benzodiazepines for the treatment of panic disorders
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18
Q

Eszopiclone and flumazenil are__________

A

hypnotics

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19
Q

Which drug used in the maintenace treatment of patients with tonic clonic or partial seizure states increases the heaptic metabolism of manu drugs including both phenytoin and warfarin?

A

Phenobarbital

  • Clonazepam and phenobabital are both used in seizure disorders
  • Chronic administration of phenobarbital increases the activity of hepatic drug metabolizing enzymes including several cytochrome P450 isozymes
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20
Q

A patient with live dysfunction is scheduled fora surgical procedure. Lorazepam or oxazepam can be used for preanesthetic sedation in this patient without special concern regarding excessive CNS depression because these drugs are _______

A

Conjugated extraheaptically

  • The elimination of most NZ involves their metabolism by liver enzymes, including cytochrome P450 isoenzymes
  • In a aptient with liver dysfunction, lorazepam and oxazepam are metabolized extraheaptically
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21
Q

benzodiazepines are barbiturates are contraindicated in ___________

A

breathing related sleep disorders

They compromise ventialtion

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22
Q

Benzodiazepines

A

ALprazolam, chlordiazepoxide, clorazepate, clonazepam, diazepam, flurazepam, lorazepam, midazolam

  • Binds GABA(a) recptor subunits to facilitate chloride channel opening and increase frequency. membrane hyperpolarization
  • Used in acute anxiety states, panic attacksm GAD, insomnia, muscle relaxation, seizure disorders
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23
Q

Benzodiazepine antagonist

A

Flumazenil

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24
Q

Barbiturate

A

Amobarbital, bitabarbital, pentobarbital, phenobarbital, secobarbital, thiopental

  • Binds to GABA(a) receptor (distinct form BZ). facilitate chloride channel opening and increase duration
  • Used in anesthesia (thiopental), insomnia, sedation, seizure disorders
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25
Q

Newer hypnotics

A

Eszopiclone, zalepton, zolpidem

  • Bind to GABA(a) receptor sites (close to BZ site). facilitates chloride channel opening
  • USed in sleep disorders especially wen sleep onset is delayed
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26
Q

Melatonin receptor agonist

A

Ramelteon

  • Activates MT1 and MT2 receptors in suprachiasmatic nucleus
  • Used in sleep disporders especiallywhen sleep onset is delayed
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27
Q

Buspirone

A

5-HT agonist

PArtial agonist and possibly D2 receptors

Used in GAD

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28
Q

A 45 year old moderately obese man has been drinking heavily for 72 hours, This level of drinking is much higher than his regular habit of drinking 1 alcoholic drink per day. his only significant medical problem is mild hypertension, which is adequately controlled by metoprolol. With this history, this man is at significant risk for

A

Cardiac arryhtmia

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29
Q

A 42 year old man with a history of alcoholism is brought to the emergency department in a condused and delirious state. he has truncal ataxia and opthalmoplegia. The most appropriate immediate course of action is to administer ______

A

Thiamine

  • Wernicke’s encephalopathy
    • delirium, gait disturbances and paralysis of the external eye muscles
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30
Q

The cytochrome p45 dependent mcirosomal ethanol oxidizing system (Meos pathway) of ethanol metabolism is most likely to be maximally activated under the condition of low concentrations of

A

NAD

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31
Q

A freshman student (70kg) attends a college party where he rapidly consumes a quantity of an alcoholic beverage that results in a blood level of 500 mg/dL. Assuming that this young man has not had an opportunity to develop tolerance to ethanol, his present cindition is best characterized as _________

A

comatose and death

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32
Q

Mechanism of action of fomepizole

A

Inhibit the emtabolic production of toxic metabolytes of methanol

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33
Q

The regular ingestion of moderate or heavy amounts of alcohol predisposes to heaptic damage after overdose of acetaminophen because chronic ethanol ingestion

A

induces hepatic-drug metabolizing enzymes

  • Chronic use of ethanol induces CYP2E1, an isozyme that converts acetaminophen to a cytotoxic metabolite. This appears to be the cause of the increased susceptibility to acetaminophen-induced heapatotoxicity
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34
Q

a 23 year old pregnant womean with alcholism presented to the emergency department in the early stages of labor. She had consumed large amounts of alcohol throughout her pregnancy. This patients infant is at high risk of a syndrome that includes

A

Mental retardation and craniofacial abnormalities

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35
Q

The combination of ethanol and disulfiram results in nausea and hypotension as a result of the accumulation of

A

Acetaldehyde

  • disulfiram inhibits acetaldehyde dehydrogenase, the enzyme that converts acetaldehyde to acetate
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36
Q

The icnrease craving experience by those who are trying to recover from chronic alcohol abuse can be ameliorated by adrug that is an

A

Anatagonist of opiod receptors (Naltrexone)

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37
Q

Naltrexone

A

Nonselective competitive anatgonist of opiod receptors

Reduced risk of relapse in individuals with alcohol use disorders

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38
Q

Acamprosate

A

Poortly understood NMDA receptor anatagonist and GABA(a) agonist effects

Reduced risk of relapse in individuals with alcohol use disorders

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39
Q

Disulfiram

A

Inhibibits acetaldehyde dehydrogenase. Causes acetaldehyde accumulation during ethanol ingestion

Deterrent to relapse in individuals with alcohol use disorders

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40
Q

Fomepizole

A

Inhibits alcohol dehydrogenase, Prevents conversion of methanol and ethylene glycol to toxic metabolites

Used in methanol and ethylene glycol poisoning

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41
Q

A 9 year old child is having learning difficulties at scholl. He has brief relapses of awareness with eyelid fluttering that occur every 5-10min. EEG studies reveal brif 3 Hz spike and wave discharges appearing synchronously in all leads. Which drug would be effecive in this child without the disadvantages of excessive sedation or tolerance development

A

Ethosuximide

  • Absence seziure
    • clonazemapam
      • CNS depressant effects
    • Ethosuximide
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42
Q

Phenytoin _______________

A

prolongs the inactivated state of Na channel

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43
Q

MOA of Benzodiazepines

A

facilitate GABA-mediated inhibitory actions

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44
Q

MOA of ethosuximide

A

selectively blocks calcium channels in thalamic neurons

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45
Q

Zonisamid eblocks ____________

A

voltage gated sodium channels

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46
Q

MOA of phenobarbital

A

produces multiple effects, mainly enhancement of GABA chlporide inhibitory activity

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47
Q

Preferred drugs for absence seizure

A

Ethosuximide and valproic acid

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48
Q

Common side effects with ethosuximide

A

GI die effects

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49
Q

Weigth ________ is common in patients on valproic acid

A

gain

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50
Q

How to reduce GI symptoms of ethosuximide?

A

Take twice a day

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51
Q

With chronic use in seizure states, the adverse effects of this drug include coarsening of facial features, hirsutism, ang gigival hyperplasia

A

Phenytoin

  • Common side effects:
    • nystagmus, diplopia, and ataxia
  • Chronic use
    • abnormalities of vitamin D metabolism, coarsening of facial features, gingival overgrowth and hirsutism may also occur
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52
Q

Abrupt withdrawal of antiseizure drugs can result in increases in seizure frequency and severity. Withdrawal is most easily accomplished if the patient is treated with

A

Ethosuximide

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53
Q

MOA of carbamazepine

A

Block if sodium ion channels

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54
Q

MOA of topiramate

A

blcok glutamate receptors

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55
Q

MOA of vigabatrin

A

inhibits GABA metabolism

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56
Q

A young man suffers from a seizure disorder characterized by tonic rigidity of the extremities followed in 15-30 secs. of tremor progressing to massive jerking of the body. This clonic phase lasts for 1 to 2 min. leaving the patient in a stupurous state. Drug msot suitable for long term management of this patient

A

Phenytoin

  • carbamazepine or phenytoin, or valproic acid
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57
Q

Cyclic ureides

A

Phenyoin, phenobarbital, ethosuximide

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58
Q

Phenytoin

A

Blocks voltage gated sodium channels

Used in GTC and partial seizures

Variable absortption, dose dependent elimination, protein binding ; many drug interactions

Toxicities: Ataxia, diplopia, gingival hyperplasia, hirsutism, neuropathy

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59
Q

Phenobarbital

A

Enhances GABA(a) receptor responses

used in GTCm and partial seizures

Long halflife, inducer of P450, many interactions

Toxicities: sedation, ataxia

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60
Q

Ethosuximide

A

Decreases calcium currents (T-type)

Used in absence seizures

Long half life

SE: Gi distress, dizziness, headache

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61
Q

Carbamazepine

A

Tricyclics

blocks voltage-fated sodium channels and decreases glutamate release

used in GTC and partial seizures

Well absorbed; active metabolite, many drug interactions

SE: ataxia, diplopia, headache, nausea

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62
Q

Benzodiazepines

A

Diazepam, lorazepam, clonazepam

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63
Q

Gabapentin

A

Blocks calcium channels

GTC and partial seizures

Variable bioavailability. Renal elimination

SE: ataxia, dizziness, somnolence

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64
Q

Pregabalin

A

Blocks calcium channels

used in partial seizures

Renal elimination

SE: ataxia, dizziness, somnolence

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65
Q

Vigabatrin

A

Inhibits GABA transaminase

used in aprtial seizures

Renal elimination

SE: drowsiness, dizziness, psychosis, ocular effects

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66
Q

Valproate

A

Blocks high frequency firing

Used in GTC and myoclonic seizures

Extensive protein binding and metabolism; many drug interactions

SE: nausea, alopecia, weight gain, teratogenic

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67
Q

Lacosamide

A

Blcoks sodium channels

Used in focal and generalized seizures

Minimal protein binding, no active metabolites

SE: dizziness, headache, diplopia

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68
Q

Lamotrigine

A

Blcoks Na and Ca channels, decreases neuronal glutamate release

GTC and partial, myoclonic, and absemces seizures

Not protein bound, extensive metabolism, many drug interactions

SE: dizziness, diplopia, headache, Rash

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69
Q

Levetiracetam

A

Binds synaptic protein SV2A, modifies GABA and glutamte release

used in GTC and partial seizures

Well absorbed, extensive metabolism, some drug interactions

Dizziness, nervousness, depression, seizures

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70
Q

Perampenel

A

Blocks glutamte AMPA receptors

Used in focal and GTC

Complete absorption, high protein binding, extensive metabolism

SE: dizziness, headache, somnolence, behavioral change

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71
Q

Retigabine

A

Activates K channels

Used in focal seizures

Moderate bioavailabilitym extensive metabolism

SE: DIzziness, somnolence, retinal changes

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72
Q

Rufinamide

A

Blcoks Na channels, other actions

Lennox-gastaut syndrome, focal seizures

Good absorption. No active metabolites

SE: somnolence, fever, diarrhea

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73
Q

Tiagabine

A

Blcoks GABA reuptake

Used in partial seizures

Extensive protein binding and metabolism some drug interactions

SE: dizziness, nervousness, depression, seizures

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74
Q

Topiramate

A

May blcok Sodium and calcium channels; also increases GABA effects

Used in GTC, absence, partial seizures, Migraine

Both hepatic and renal clearance

SE: sleepiness, cognitive, slowing, confusion, paresthesias

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75
Q

Zonisamide

A

Blcoks sodium channels

Used in GTC, aprtial and myoclonic seizures

Bith heaptic and renal clearance

SE: sleepiness, cognitive slowing, poor concentration, paresthesias

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76
Q

Agents with low blodd:gas solubility have ________onset of action

A

Faster

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77
Q

Chest muscle rigidity often follows the administration of ________

A

fentanyl

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78
Q

______ has antiemetic effect

A

Propofol

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79
Q

Halothate and other inhaled anesthetics causes ________

A

Bronchodilation

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80
Q

_________ is assocaited with muscle twithcing

A

Enflurane

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81
Q

A 23 year old man has pheochromocytoma. Which agent should be avoided?

A

Isoflurane

  • Isofluranse sensitizes the myocardium to catecholamines as does halothane
  • Arrythmias may occur
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82
Q

Least potent of the inhaled anesthetics

A

nitrous oxide

  • lacks cardiovascular depression
  • eliminated via the lungs
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83
Q

MAC

A
  • Methoxyflurane has an extremely low MAC value
  • Inversely related to potency
  • gives no information about the slope of the dose-response curve
  • Use of opiod analgesics or other CNS depressants lowers the MaC value
  • elderly patients are more sensitive, so MAC value are lower
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84
Q

Fentanyl protocol

A
  • Fentanyls effects can be reversed with naloxone after the procedure
  • widely used in cardiac surgeries
  • skeletal muscle rigidity than relaxation
  • The additon of vasodialtors or a Beta blocker may be needed to prevent intraoperative hypertension
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85
Q

Malignant hyperthermia

A
  • occur during general anesthesia with halogenated anesthetics and skeletal muscle relaxants
  • succinylcholine and tubocurarine
  • Release of calcium from skeletal sarcoplasmic reticulum leads to msucle spasms, hyperthermiam and autonomic instability
  • Clinical myopathy associated with mutations in the gene loci for the skeletal muscle ryanodine receptor or L-type calcium receptors
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86
Q

Drug of choice for malignant hyperthermia

A

Dantrolene

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87
Q

If ketamine is used as the sole anesthetic in the attempted reduction of a dislocated shoulder joint, its actions will include

A

Analgesia

  • cardiovascular stimulant
  • increasing heart rate and BP
  • central sympathetic stimulation from inhibition of norepinephrine reuptake sympathetic nerve endings
  • Analgesia
  • Amnesia
  • preservation of muscle tone and minimal depression of respiration
88
Q

Inhaled anesthetics

A

Desflurane, Enflurane,Halothane,Isoflurane,sevoflurane,Nitrous oxide

Faciliatte GABA mediated inhibition, block brain NMDA and ACHn receptors

Increase cerebral blood flow. ENFLURANE and HALOTHANE decrease cardiac output. Others cause vasodilation. All decrease respiratory functions - Lung irritation (desflurane)

Rate of onset and recovery vary by blood:gas partition coefficent. recovery mainly due to redistribution from brain to blood and thence to alveolar air and other tissues

89
Q

Thiopental/tioamylal/methohexital

A

Barbiturates

Facilitate GABA-mediated inhibition of GABA(a) receptors

Circulatory and respiratory depression. decrease intracranial pressure

High lipid solubility-fast onset and short duration due to redistribution

SE: extension of CNS depressant actions. additive CNS depression with many drug

90
Q

Midazolam

A

Facilitates GABA-mediated inhibition at GABA(a) receptors

Less depressant than barbiturates

SLower onset,but longer duration than barbiturates

SE: post op respiratory depression reveresed by flumazenil

91
Q

Ketamine

A

Blocks excitation by glutamate at NMDA receptors

Analgesia, amnesia, and catatonia but consciousness retained. Cardiovascular stimulation

Moderate duration of action - hepatic metabolism

SE: increased intracranial pressure. emergence reactions

92
Q

Etomidate

A

Faciliatets GABA-mediated inhibition at GABA(a) receptors

Minimal effects on CV and respiratory functions

Short duration due to redistribution

No analgesia, paim on injection (may need opiod), myoclonus, nausea, and vomiting

93
Q

Opiods

A

fentanyl, alfentanil, ramifentanil, morphine

Interact with u, k, and delta receptors

Marked analgesia, respiratory depression

Alfentanil and ramifentanil fast onset (induction)

Respiratory depression - reversed by naloxone

94
Q

Phenols

A

Propofol, fospropofol

Vasodialtion and hypotension. negative inotropy, fospoprofol water soluble

Fast onset and fast recovery due to inactivation

Hypotension(during induction), cardiovascular depression

95
Q

Characteristics properties of local anesthetics

A
  • Increase in membrane refractory period
  • Blockade of voltage dependent sodium channels
  • Effects of vascular tone
  • Slowing of axonal impulse condition
96
Q

The pKa of lidocaine is 7.7. Infected tissue, which can be acidic, for example at pH 6.7, the percentage of the drug in the nonionized form will be

A

10%

  • Because the drug is a weak base, it is more ionized at pH values lower than its pKa. Because the pH given is 1 log unit lower (more acid) thean the pKa, the ratio will be approximately 90:10
97
Q

Speed of onset of nerve blcokage is _______ in myelinated fibers

A

faster

98
Q

The most important effect of inadvertent IV administration of a large dose of lidocaine is

A

Seizure

99
Q

Factors that influence the action of local anesthetics

A
  • Blood flow through the tissue
  • Dose of local anesthetic injected
  • The use of vasoconstrictors
  • Tissue pH
100
Q

You have a vial containing 10 mL of a 2% solution of lidocaine, How much lidocaine is present in 1mL

A

20 mg

101
Q

In overdosage ___________ (with oxygen) is helpful to correct acidosis and lower extracellular potassium

A

hyperventilation

102
Q

A vasoconstrictor added to a solution of lidocaine for a peripheral nerve block will

A

Decrease the risk of seizure

Increase the duration of anesthetic

103
Q

A child requires multiple minor surgical procedures involving the nasopharynx, Which drug has high surface local anesthetic activity and intrinsic vasoconstrictor actions that reduce bleeding in mucous membranes

A

Cocaine

104
Q

Prilocaine is relatively contraindicated in patients with cardiovascular or pulmonary disease because the drug

A

Causes decompensation through formation of methemoglobin

105
Q

Amides

A

Articaine, Bupivacaine, Levobupivacaine, lidocaine, mepivacaine, prilocaine, ropivacaine

Blockade of Na channels. slows, the prevents action potential propagation

Hepatic metabolism via CYP450 in part. Half lives: lidocaine, prilocaine <2h others 3-4hours

Analgesia via topical use or injection

106
Q

Esters

A

Benzocaine, cocaine, procaine, tetracaine

Blockade of sodium channels, slows then prevents action potential propagation. Plus cocaine has intrinsic sympathomimetic actions

Rapid metabolism via plasma esterases. Short half-lives

Analgesia, topical only for cocaine and benzocaine

107
Q

Characteristics of phase I depolarizing neuromuscular blockade due to succinylcholine

A

Sustaimed tension during period of tetanic stimulation

108
Q

The main reason for administering atropine was to

A

Block cardiac muscarinic receptors

  • Acetylcholinesterase inhibitors used for recersing effects of nondepolarizing muscle relaxants cause increases in ACh
  • Atropine is effective, glycopyrrolate is usually preferred because it lacks CNS effects
109
Q

A muscarinic receptor antagonist would probably not be needed when a cholinesterase inhibitor was given for reversal of skeletal muscle relaxant actions of a non depolarizing drug if the NM blocking agent used was

A

Pancuronium

  • it can bloick muscarinic receptors, especially those in the heart
  • Caused bradycardia and hypertension and may cause dysrhythmias
110
Q

Most effective emergent managment of malignant hyperthermia

A

Dantrolene

  • interacts with the RyR1 channel to block the release if activator calcium
111
Q

The clinical use of succinylcholine, especially in patients with diabetes is associated with

A

Aspiration of gastric contents

  • Fasciulations associated with succinylcholine may increase intragastric oressure with possible complication sof regurgitation
  • patients with delayed gastric emptying such as those with esophageal dysfunction or diabetes
112
Q

Which drug is most often assocuated with hypotension and is related to clonidine

A

Tizanidine

  • causes hypotension via a2-adrenoceptor
113
Q

Spasmolytic durgs

A
  • Cyclobenzaprine decreases both oropharyngeal sectrions and gut motility
  • Dantrolene has no significant effect on the release if calcium from sarcoplasmic reticulum in cardiac muscle
  • Diazepam causes sedation at doses commonly used to reduce muscle spasms
  • Intrathecal use of baclofen in effective in some refractory cases of muscle spasticity
  • Baclofen activates GABA(b) receptors in the SC, these receptors are coupled to K channels
114
Q

Which drug is most likely to cause hyperkalemia leading to cardiac arrest in patients with spinal cord injuries

A

Baclofen

  • Skeletal muscle depolarization by succinylcholine releases potassium from the cellsm and the ensuing hyoerkalemia can be life threathening in terms of cardiac arrest]
  • Most susceptioble
    • extensive burns
    • spinal cord injuries
    • neurological dysfunction
115
Q

Which drug has spasmolytic activity and could also be used in the management of seizures caused by overdose of a local anesthetic

A

Diazepam

  • Both antiseizure and spasmolytic
  • Cyclobenzaprine is used for acute local spasm and has no antiseizure activity
116
Q

Myalgias are common postoperative complaint of patients who receive large doses of succinylcholine. possibly the result of muscle fasciculations caused by depolarization. WHich drug administered in the opening room can be used to prevent postoperative pain caused by succinylcholine?

A

Atracurium

117
Q

Succinylcholine

A

Agonist at ACH(n) receptors causing intitial twitch then persistent depolarization

Stimualtes ANS ganglia at M receptors

Pareneteral: short action, inactivated by plasma esterases

SE: muscle pain, hyperkalemia, increased intragastric and intraocular pressure

118
Q

Nondepolarizing Skeletal muscle relaxants

A

d-tubocurarine, Atracurium, Cisatracurium, Mivacuurium, rocuronium, vecuronium

Competitive anatagonists at skeletal muscle ACh-N receptors

ANS ganglion block(Tubocurarine). Cardiac M block(pancuronium)

Parenteral use, variable disposition; Spotaneous inactivation (Atracurium, cisatracurium); metabolism by plasma ChE (mivacurium) ; hepatic metabolism (rocuronium, vecuronium); Renal elimination (doxacurium, pancuronium, tubocurarine)

SE: Histamine release (Mivacurium, Tubocurarine); Laudanosine formation (Atracurium); muscle relaxation is potentiated by inhaled anesthetics, aminoglycosides and possibly quinidine

119
Q

Centrally acting Skeletal Msucle Relaxants

A

Baclofen, Cyclobenzaprine, iazepam, tizanidine

120
Q

Baclofen

A

Facilitates spinal inhibition of motor neurons

Pre-and postsynaptic GABA(b) receptor activation

Oral; intrathecal for severe spasticity

SE: sedation, muscle weakness

121
Q

Cyclobenzaprine

A

Inhibition of spinal stretch reflex

Oral route for acute muscle spasm due to injury or inflammation

SE: M block, sedation, sonfusion, and ocular effects

122
Q

Diazepam

A

Facilitates GABA-ergic transmission in CNS

GABA(a) receptor activation: postsynaptic

Oral and parenteral for acute and chronic spasms

SE: sedation, additive with other CNS depressants; abuse potentials

123
Q

Tizanidine

A

Pre and postsynaptic inhibition

alpha 2 agonist in spinal cord

Oral for acute and chronic spasms

SE: muscle weakness, sedation, hypotension

124
Q

Dantrolene

A

Direct-acting

Weakens muscle contraction by reducing myosin-actin interaction

Blocks RyR1 Calcium channels in skeletal miscle

Oral for acute and chronic spasm. IV for malignant hyperthermia

SE: muscle weakness

125
Q

Ancipated action of levodopa

A
  • Dizziness may occur, especially when standing
  • Take the drug in divided doses to avoid nausea
  • The drug will probably improve his symtpoms for a period of time but not indefinitely
  • Uncontrollable muscle jerks may occur
126
Q

Livedo reticularis is an adverse effect of ________

A

Amantadine

127
Q

Fluctuates in its effectivieness with increasing frequency as treatment continues

A

Levodopa

128
Q

Pramipexole is a dopamine ___________ receptor acrivator and does not require bioactivation

A

D3

  • excreted in unchanged form
129
Q

Drugs that ____________can exacerbate dyskinesia in a patient taking levodopa

A

activate dopamine receptors

130
Q

True or false. Muscarinic receptor blcokers prevent occurence of dyskinesia

A

False

131
Q

a 51 year old patient with parkinsonism is being maintained on levodopa-carbidopa with adjunctive use if low doses of tolcapone but continues to have off periods of akinesia. A drug used to rescue the patient that provides temporary relief

A

Apomorphine

  • Pretreatment with the antiemetic trimethobenzamide for 3 days us essential to prevent severe nausea
132
Q

_______causes mydriasis and may precipitate an acute attack if glaucoma

A

Levodopa

133
Q

true or false. Antimuscarinic drugs may improve the tremor and rigidity

A

true

134
Q

A previously healthy 40 year old woman begins to suffer from slowed mention, lack of coordination, and brief weithing movements of her hands that are not rhythmic. In addition, she has delusion of being persecuted. The woman has no history of psychiatric or neurologic disorders but several relatives have had similar symptoms. Although further diagnostic assessment should be made, it is very likely that the most appropriate drug for treatment will be

A

Haloperidol

135
Q

true or false. Pramipexole is an egot derivative

A

False

136
Q

Tolcapone may be of value in patients being treated with levodopa-carbidopa because it _______

A

Decreases the formation of 3-O methyldopa

137
Q

Ropinirole act on the _______receptor

A

D2

138
Q

Which of the following drugs is most suitable for management of essential tremor in a patient who has pulmonary disease

A

Metoprolol

139
Q

Levodopa/carbidopa

A

PRecursor of dopamine. Carbidopa inhibits peripheral metabolism via dopa decarboxylase

Primary drug used in parkinson’s disease

Oral COMT and MAO type B inhibitors allow smaller doses and prolong actions. Duration of effects: 6-8 h

SE: GI upsets, dyskinesias, behavioral effects. On and Off phenomenon

140
Q

Dopamine Agonists

Pramipexole, ropirinole, apomorphine, rotigotine,bromocriptine

A
  • D2 agonists (Apomorphine, bromocriptine, rotigotine,ropinirole)
  • D3 Agonist (pramipexole)
  • Pramipexole, rotigotine and ropinirole
    • sole agents in early parkinson’s disease and adjunct to L-dopa
  • Apomorphine
    • Rescue therapy
  • Oral: pramipexole; SHort halflife, renal elimination
  • Ropinirole, CYP1A2 metabolism, drug interactions possible
  • rotigotine: transdermal
141
Q

MAO inhibitors

Rasagiline, Selegiline, Safinamide

A

Inhibit MAO type B

Rasagiline, selegiline - adjunctive with L-dopa ; safinamide to reduce on-off phenomena

Oral. Half-lioves permit bid dosing

SE: Serotonin syndrome with meperidine and possibly SSRIs and TCAs

142
Q

COMT Inhibitors

Entacapone, Tolcapone

A

Block L-dopa metabolism in periphery (bith) and CNS dopamine (tolcapone)

Prolongs L-dopa actions

Oral

143
Q

Benztropine

A

Antimuscarinic agent

Improves tremr and rigidity not bradykinesia

Oral: once daily

144
Q

Drugs of Hungtington’s disease

Tetrabenazine, Reserpine, Haloperidol

A
  • Tetrabenzine, reserpine : Depeltes amines
  • Haloperidol: D2 antagonist

Reduce symptom severity

Oral

  • Side effects
    • Tetrabenzine, reserpine : Depression, hypotension, sedation
    • Haloperidol : Extrapyramidal dysfunction
145
Q

Drugs for tourette syndrome

A
  • Haloperidol
    • D2 receptor blockers
    • reducel vocal and motor tic frequency
    • Oral
    • SE: Extrapyramidal dysfunction
  • Clonidine
    • alpha 2 blocker
    • oral
146
Q

Pathologic basis of schizophrenia

A

Drug-induced psychosis can occur without activation of brain dopamine receptors

  • Dopamine receptor blockers cause EPS
147
Q

trifluoperazine was prescribed for a young male patient diagnosed as suffering from schizophrenia. He complains about the side effects of his medication. Which of the ff is not likely to be one of his complaints

A. Constipation

B. Decreased Libido

C. Excessive Salivation

D. Postural hypotension

A

C

  • Phenothiazine causes sedation and are antagonist at muscarinic and alpha drenoceptors
    • postural hypotension
    • blurring of vision
    • dry mouth
148
Q

retinal pigmentation is a dose dependent toxic effect of _________

A

thiorizadine

149
Q

_______ exacerbate tardive dyskinesia

A

Atropine and other muscarinic blockers

150
Q

Akathisias may be relieved by ________ the dosage

A

Decreasing

151
Q

Haloperidol is not an appropriate drug management for ______

A. Acute mania

B. Amenorrhea-glactorrhea syndrome

C. Phencyclidine intoxication

D. Schizoaffective disorders

E. Touretter sybdrome

A

B.

152
Q

Lithium dosage may need to be ________ in patients taking thiazides

A

Decreased

  • slow onset
153
Q

_________urinary sodium inhibits renal tubular reabsorption of Lithium

A

High

154
Q

A 30 year old male patient on drug therapy for a psychiatric problem. He complains that he feels “flat” and that he gets confused at times. He has been gaining weight andnhas lost his sex drive, As he moves his hands, you notice a slight tremor. He tells you that since he has been on medication he is always thirsty and frequently has to urinate. The drug he is most likely taking is ?

A

Lithium

155
Q

A young woman recentley diagnosed as schizophrenic develop severe muscle cramos with torticollis, a short time after drug therapy is initiated with haloperidol. The best course of action would be

A

Inject benztropine

156
Q

Drug with established to be both effective and safe to use in pregnant patient suffering from bipolar disorder

A

Olanzepine

157
Q

A drug that has a high affinity for 5-HT2 receptors in the brain, does not cause EPS or hematoxicity, but is reported to increase the risk of significant QT prolongation?

A

Ziprasidone

158
Q

PHENOTHIAZINES

(chlorpromazine, Fluphenzine,Thioridazine)

A

Block of D2 receptors >>> 5-HT2 receptors

Blocks alpha, M, and H1 receptors. Sedation, Decreas seizure threshold

Used in Schizophrenia, Bipolar disorder (Manic phase), antiemesis, preop sedation

Oral and parenteral forms, hepatic metabolism, long half life

SE: Extensions of alpha and M receptr blocking. EPS, tardive dyskinesias, hyperprolactinemia

159
Q

THIOXANTENE

(Thiothixene)

A

Similar to phenothiazones

Used in schizophrenia

less risk of tardive dyskinesia

160
Q

BUTYROPHENONE

(haloperidol)

A

Block of D2 receptors >>> 5 HT2 receptors

Some alpha block. less M block and sedation than phenothiazines

Used in Schizophrenia, bipolar disorders (manic phase), Huntington’s choreat, Tourette

Oral and parenteral forms. Heaptic metabolism

SE: EPS (Major)

161
Q

SECOND GENERATION

(Aripiprazole, clozapine, olanzapine, quetiapine, risperidone, ziprasidone)

A

Block of 5-HT2 receptors >> D2 receptors

Some alpha block (Clozapine,risperidone, ziprasidone) and M block (clozapine, olanzapine), variable H1 Block

Ued in Schizophrenia (positive and negative symptoms), bipolar disorder (Olanzapine, risperisone), MDD (aripiprazole), agitaion in Alzheimer’s andParkinson’s\

SE: Agranulocytosis (clozapine), diabetes and weight gain (clozapine ,olanzapine), hyperolactinemia (risperidone), QT prolongation (Ziprasidone)

162
Q

Lithium

A

Uncertain, suppresses IP3 and DAG signalling

No specific actions on ANS receptors or specific CNS receptors. No sedation

Used in Bipolar affective disorder. prevents mood swings (prophylaxis)

Renal elimiantion, halflife (20h), narrow therapeutic window, clearance decreased by thiazide and NSAIDs

SE: tremor, edema, hypothyroidism, renal dysfunction, pregnancy category D

163
Q

Alternative drugs for bipolar affective disorder

(Carbamazepine, lamotrigine, Valproic acid)

A

Unclear actions in bipolar disorder

Ataxia and diplopia (carbamazepine), Nausea, dizziness, and headache (lamotrigine), GI distress, weigh gain, alopecia (valproic acid)

Valproic acid competes with lithium as firsth choice in BPD, acute phase. Others also used in acute phase and for prophylaxis in depressive phase

Carbamazepine forms active emtabolite (phase 1); lamotrigine and valproic acid form conjugates (phase II)

SE: Hematotoxicity and induction if drug metabolism (carbamazepine). Rash (lamotrigine), Hepatic dysfunction, weight gain, and inhibition of drug metabolism (Valproic acid)

164
Q

A 36 year old woman with symproms of MDD. She is not currently taking any prescription. She was given sertraline. In your informtation to the patient, you will tell that

A
  • Sertaline may take 2 weeks or more to become effective
  • Preferable to take the drug in the morning
  • Muscle cramps and twitches can occur
  • She should notify you if she anticpates using other prescription medications
165
Q

Chronic treatment with __________ leads to downregulation of adrenoceptors in the CNS

A

TCA

166
Q

Selegiline is a selective inhibitor of ___________

A

MAO-B

167
Q

Nefazodome is a highly selective antagonist at the _________receptor

A

5-HT2

168
Q

A 34 year old man who was prescribed citalopram for depression has decided he wants to stop taking the drug, WHen questioned, he sait that it was affecting his sexual performance. You ascertain that he is also trying to overcome his dependency on tocacco products. If you decide to reinstiture drug therapym the best choice would be

A

Buprion

  • SSRIs and venlafacine causes sexual dysfunction
    • TCA may also decrease libido
169
Q

_____ are effective in depresssions with attendant anxiety, phobi features and hypochondriasis

A

MAO inhibitors

170
Q

True about Imipramine overdose

A
  • Administer bicarbonate and potassium chloride (to correct acidosis and hypokalemia)
  • Adminsiter lidocaine (to control cardiac arrythmias
  • Maintain heart rhythm by electrical apcing
  • Use IV diazeoam to control seziures
  • Hemodialysis is not helpful
171
Q

Which drug is an antagonist at 5-HT2 receptors and widely used for the management of insomnia in depressed patients

A

Trazodone

172
Q

Ideal drug to be given to elderly patients with depressive symptoms

A

Citalopram

173
Q

SSRIs are much less effective than TCA in the management of

A

Chronic neuroathic pain

174
Q

Drug that is most likely tobe of value in OCD

A

Clomipramine

175
Q

To be effective in breast cancer, tamoxifen must be converted to an active fotm by CYP2D6. Cases of inadequate treatment when tamoxifen was administered with

A

Fluoxetine

176
Q

TCAs

(amitriptyline, clomipramine. Imipramine)

A

Blcok NE and 5-HT transportes

Used in MDD, OCD, chronic pains

CYP substrates; interactions with inducers and inhibitors. Long half lifr

177
Q

SSRIs

(Citalopram, fluoxetine, paraxetine, sertaline)

A

Blcok 5-HT transporters

Used in MDD, anxiety disorders, OCD, MDD, PTSD, bulimia

CYP2F6 and 3A4 inhibitors (fluoxetinem paroxetine). 1A2 (fluvoxamine). Half life 15h

SR: severe dehydration

178
Q

5-HT2 antagonists

(Nefazodone, trazodone)

A

Blocks 5-Ht2 receptors

MDD, hypnosis (trazodone)

Usually required bid dosing. CYP3A4 inhibitor

SE; sedation. modest alpha and H1 blockade (trazodine)

179
Q

Heterocyclics

(Amoxapine, buprioprion, maptrotilline, mirtaxapine)

A

Mirtazapine blocks MOA-A and B. Selegiline more active vs MAO-B

Used in MDD, smoking cesasation (bupropriom), sedation (mirtazapone)

Extensiven heaptic metabolism. CYD2D6 inhibition *bupropion)

SE: lowers seizire threshold (Amaxapine, Bupropion). Seadtion and wait gain (mirtazapine)

180
Q

MAO inhibitors

(Isocaboxazod, phenelzine, selegiline)

A

Inhibi MAO -A and B ; selegiline more active vs MAO-B

Used in MDD and unresponsive to other drugs

Hypetension with tyranine, ANd sympathomimectis. Serotonin syndrome if combine with ssris. If combined with ssris. very long hafl lives

SE:hypotension, insomnia

181
Q

Patient is a cancer patient currently on oxycodone plus acetaminophen taken orally. Despite increasing doses of the analgesic combiantion, the pain is getting worseThe most appropriate oral medication for his increasing pain is

A

Hydromorphone

  • Pain associated with metastatic carcinoma ultimately necessitates the use of an opiod analgesic that is equivalent in strength to morphine
    • hydromorphone
    • oxymorphone
    • levorphanol
182
Q

Tolerance will not develop to a significant extent with respect to _____________

A

Pupillary constriction

183
Q

You are on your way to take an examination and you suddenly get an attack of diarrhea. If you stop a nearby drugstore for an over the counter opiod with antidiarrhea action, you will be asking for

A

Loperamide

184
Q

An emergency department patient with severe pain thought to be of GI origin received 80 mg of meperidine. She subsequently developed a severe reaction characterized by tachycardia, hypertension, hyperpyrexia and seizures. Questioning revealed that the patient had been taking a drug for psychiatric condition. Which drug is most likely to be responsible for this untoward interaction with meperidine?

A

Phenelzine

Concomitant administration of meperidine and monoamine oxidase inhibitors such as isocarboxazid or phenelzine has resulted in life threatening hyperpyrexic reaction that may culmiante in seizures or coma

Concomitant use of selective serotonin reuptake ihibitors and meperidine has resulted in the serotonin syndrome

185
Q

Genetic polymorphisms inc ertain hepatic enzymes involved in drug metabolism are established to be responsible for variations in analgesic response to ___________

A

Codeine

  • Codeine, hydrocodone, and oxycodone are metabolized by CYP2D6 and variations in analgesic response to the drugs have been attributed to genetic polymorphisms in this isozyme
186
Q

A yound man is brought to the emergency department in an anxious and agitated state. He informs the attending physician that he usues “street drugs” and that he gave himself an IV “fix” approximately 12h ago. After an initial period of contenment and relaxation, he has now has chills and muscle aches and has also been vomiting. His symptoms include hyperventilation and hyperthermia. The attending physician notes that his pupil size is larger than normal

A

The sign and symptoms are those of opiod abstinence

Methadone should be given

Beneficial action of diazepam are restricted to the relief of anxiety and agitation

187
Q

Which statement about nalbuphine is most accurate??

A

Response to naloxone in overdose may be unreliable

188
Q

Which drug does not activate opiod receptors, has been proposed as maintenance drug in treatment programs for opiod addicts. and with a single oral dose, will block the effects of injected heroin for up to 48 hours

A

Naltrexone

189
Q

Which drug is a full agonist at opiod receptors with analgesic activity equivalent to morphine, a longer duration of action, and fewer withdrawal signs on abrupt discontinuance than morphine?

A

Methadone

  • Fentanyl, hyrodmorphone, and methadone are full agonists with analgesic efficacy similar that of morphine
190
Q

Strong agonists

(fentanyl, Hydromorphone, meperidine, morphine, methadone, oxymorphone)

A

Strong mu agonists. variable delata and kappa agonists

Used in severe pain, anesthesia (adjunctive). Dependence maintenance (methadone)

Hepatic metabolism. Duration: 1-3 h (methadone 4-6h)

SE: respiratory depression, constopation, addiction liability

191
Q

Parial agonists

(Codeine, hydrocodone)

A

mu agonists, VAriable delta and kappa agonists

Used in mild to moderate pain; cough (codeine). Analgesic combinatios with NSAIDs and acetaminophen

Genetic variations in metabolism

SE: Respiratory depression, constipation, addiction liability (weaker effects)

192
Q

Buprenorphine

A

Mixed agonist-antagonist

Partial mu agonist and kappa antagonist

Used in moderate to severe pain. Dependence maintenance, reduces craing for alcohol

Long duration

193
Q

Nalbuphine

A

Mixed agonist-antagonist

Kappa agonist and mu antagonist

Used in mdoerate to severe pain

Parenteral only

194
Q

Opiod antagonist

(Naloxone, Naltexone,nalmefene)

A

Antagonists at all opiod receptors

Used in opiod overdose. Dependence maintenance (naltexone )

Duration: naloxone 2h. Naltrexone and nalmefene >10h

SE: rapid antagonism of all opiod actions)

195
Q

Antitussives

(codeine, dextromethorphan)

A

Mechanism uncertain. Weak mu agonist, Inhibits NE and 5-HT transporters

Used in acute debilitating cough

Duration: 0.5-1h

SE: reduces cough reflex. Toxic in overdose

196
Q

Tramadol

A

Weak mu agonist. Blocks serotonin reuptake.

Used in mdoerate pain. ASjunctive to opiods in chronic pain states.

Duration: 4-6h

SE: toxic in overdose (seizures)

197
Q

Antagonists of peripheral opiod action

(methylnaltrexone, alvimopan, naloxegol)

A

Peripheral antagonistm of mu receptors

Used in treatment of opiod induced constipation, postoperative ileus

Do not enter the CNS. DUration: variable

SE: similar to peropjera; toxicities of morphine

198
Q

True about Alprazolam

A
  • Abrupt discontinuance of alprazolam after 4 weeks of treatment may eleicit withdrawal signs
  • Additive CNS depression occurs with Ethanol
  • Most benzodiazepines are Schedule IV-controlled drugs
  • Tolerance can occur with chronic use of any benzodiazepine
199
Q

Schedules of controlled drugs

A
  • I - no medical ise; high addicition potential
    • Flunitrazepam, heroin, LSD, mescaline, PCP, MDA, MDMA, STP
  • II - Medical use; high addiction potential
    • Amphetamines, cocaine, methylphenidate, short acting barbiturates, strong opiods
  • III - Medical use; moderate abuse potential
    • anabolic steroid, barbiturates, dronabinol, ketamine, mdoerate opiod agonists
  • IV - Medical use; low abuse potential
    • benzodiazepines, chloral hydrate, mild stimulants, most hypnotics (zaleplon, zolpidem), weak opiods
200
Q

Which drug, a partial agonist at nicotinic acetylcholine receptors is used in smoking cessation programs but may cause seizures in overdose?

A

Verenicline

  • Acamprosate
    • antagonist of NMDA glutamate receptors
      • used together with counseling in alcohol treatment programs
201
Q

Abuse of opiod analgesic

A
  • Symptoms usually begin within 6-8 h and the acute course may last 6-8 days
  • Lacrimation, rhinorrhea, yawning, and sweating are early signs
  • Secondary phase of heroin withdrawal
    • bradycardia, hypotension, hypothermia, and mydriasis may last 26-30 weeks
  • Clonidine may be useful in reducing symtoms caused by sympathetic overactivity
  • Methadone alleviates most of the symptos of heroin withdrawal
  • Naloxone may precipiate a severe withdrawal state in abusers of opiod analgesics with symptoms starting in less than 15-30 min
202
Q

Intravenous cocaine overdose causes _______

A

Tachycardia, agitation, hyperthermia, MI, seizures

203
Q

Dilated pupils and tachycardia are characteristic effects of ______________

A

scopolamine

204
Q

_____ Acts as a positive reinforcer of self adminsitration in animals

A

PCP

205
Q

The inhalation of ______ is likely to cause headache, hypotension, and flushing

A

isobutyl nitrite

206
Q

_____ and _____ are the most widely abused opiods by medical personnel

A

Fentanyl and meperidine

207
Q

Sign or symptom most likely to occur with marijuana>

A

Conjunctival reddening

208
Q

A college student us brought to the emergency department by friends. The student had taken a drug and then went Crazy. The Patient is agitated and delirious, Several persons are required to hold him down. His skin is warm and sweaty. and his pupils are dilated. Bowel sounds are normal. SIgns and symptoms include tachycardia, marked hypertension, hyperthermia, increased muscle tone, and both horizontal and vertical nysgtagmus

A

Phencyclidine

  • Management:
    • ventilarory support and control of seizures (with a benzodiazepine, hypertension and hyperthermia
    • Antipsychotic drugs (haloperidol) may also be useful for psychosis
    • Acidificication of urine
209
Q

Opiod antagonists

(Naloxone, Naltrexone)

A

Reverse or block effects of opiods

Naloxone - opiod overdose; Short half life (1-2h)

Naltrexone - Treatment of alcoholism (like morphine -4h)

210
Q

Methadone

A

Synthetic opiod

Slow acting agonist at mu opiod receptors

Acute effects like morphine

Used in substitution therapy for opiod addicts

Variable but longer halflife. ToxicityL like morphine reagarding acute and chronic effects including withdrawal

211
Q

Buprenorphine

A

Partial mu receptor agonist

Attentuates acute effects of morphine and other strong opiods

Substitution therapy for opiod addicts

Long half-life (>40h). Formulated with nalorphine to avoid illicit IV use

212
Q

Varenicline

A

N-receptor partial agonist.

Agonist at ACH(n) receptor subtype

Blocks rewarding effects of nicotine

SMoking cessation

SE: Nausea and vomiting, psychiatric changesm seizeures in high dose

213
Q

Oxazepam, lorazepam

A

Benzodiazepines

Modulators of GABA(a) receptors.

Enhance GABA functions in CNS

Attenuate withdrawal symptoms including seizures from alcohol and other sedative-hyptonics

Half-life 4-15 h; lorazepam kinetics not affected by liver dysfunction

214
Q

Acomprosate

A

Antagonist at glutamate NMDA receptors

May blcok synaptic plasticity

Treatement of alcoholism (in combination with counseling)

SE: allergies, arrythmias,variable BP effects, headache and impotence. Hallucination in elderly

215
Q

Rimonabant

A

Inverse agonist at CB1 receptors

Decrease GABA and glutamate release in CNS

Treatment of obesity. Off label use for smoking cessation

Major depression. Increased suicide risk

I hate DRUGS!! (26 decks)

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