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CNS Pathology > Analgesic, Sedative and Anesthetic Pharmacology > Flashcards

Analgesic, Sedative and Anesthetic Pharmacology Flashcards

1
Q

What is the mechanism of opioid analgesics?

A

Act as agonists at opioid receptors to modulate synaptic transmission (open K+ channels, close Ca2+ channels to decrease synaptic transmission)

Inhibit release of ACh, NE, 5-HT, glutamate and substance P

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2
Q

Clinical use of opioid analgesics

A

Pain

Acute pulmonary edema

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3
Q

Which opioid class drug is used for cough suppression?

A

Dextromethorphan

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4
Q

Which opioids are used for diarrhea?

A

Loperamide

Diphenoxylate

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5
Q

Which opioid is used for maintenance programs for addicts?

A

Methadone

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6
Q

Toxicity of opioids

A

Addiction

Respiratory depression

Constipation

Miosis

Additive CNS depression with other drugs

Tolerance does not develop to miosis and constipation

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7
Q

Tx for opioid toxicity

A

Naloxone

Naltrexone

Opioid receptor antagonists

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8
Q

Mechanism of butorphanol

A

Mu-opioid receptor PARTIAL agoinst and kappa-opioid receptor agonist

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9
Q

Clinical use of butorphanol

A

Severe pain (migraine, labor, etc)

Causes less respiratory depression than full opioid agonists

Produces analgesia

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10
Q

Toxicity of butorphanol

A

Can cause opioid withdrawal symptoms if patient is also taking full opioid agonist (competition for opioid receptors)

Overdose not easily reversed with naloxone

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11
Q

Mechanism of tramadol

A

Very weak opioid agonist

Also inhibits serotonin and NE reuptake (works on multiple neurotransmitters – "tram it all" in with tramalol)

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12
Q

Clinical use of tramadol

A

Chronic pain

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13
Q

Toxicity of tramadol

A

Similar to opioids

Decreases seizure threshold

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14
Q

Mechanism of phenytoin

A

Use-dependent blockade of Na+ channels; inhibition of glutamate release from excitatory presynaptic neurons

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15
Q

Clinical use of phenytoin

A

Tonic-clonic seizures

Also a class 1B antiarrhythmic

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16
Q

Toxicity of phenytoin

A

Nystagmus

Diplopia

Sedation

SLE-like syndrome

Induction of Cyt P-450

Chornic use produces gingival hyperplasia, peripheral neuropathy, hirsutism, and megaloblastic anemia

Teratogenic

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17
Q

What class of drugs are phenobarbital, pentobarbital, thiopentla and secobarbital?

A

Barbiturates

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18
Q

Mechanism of phenobarbital, pentobarbital, thiopentla and secobarbital (barbiturates)?

A

Facilitate GABAA action by increasing duration of Cl- channel opening

Thus decreases neuron firing

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19
Q

Contraindication for phenobarbital, pentobarbital, thiopentla and secobarbital (barbiturates)?

A

Porphyria

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20
Q

Clinical use of phenobarbital, pentobarbital, thiopentla and secobarbital (barbiturates)?

A

Sedative for anxiety

Seizures

Insomnia

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21
Q

Which barbiturate is used for induction of anesthesia?

A

Thiopental

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22
Q

Toxicity of phenobarbital, pentobarbital, thiopentla and secobarbital (barbiturates)?

A

Respiratory and cardiovascular depression (can be fatal)

CNS depression

Dependence

Drug interactions (induces P-450)

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23
Q

Tx for phenobarbital, pentobarbital, thiopentla and secobarbital (barbiturates) overdose

A

Overdose treatment is supportive (assist respiration and maintain BP)

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24
Q

Mechanism of benzodiazepines

A

Facilitate GABAA action by increasing frequency of Cl- channel opening

Decrease REM sleep

Most have long half lives and active metabolites

25
Q

Clinical use of benzodiazepine

A

Anxiety

spasticity

Detoxification (esp alcohol withdrawals)

Night terrors

Sleepwalking

General anesthetic

Hypnotic

26
Q

Toxicity of benzodiazepine

A

Dependence

Additive CNS depression effects with alcohol

Less risk of respiratory depression and coma than with barbiturates

27
Q

Tx of benzodiazepine overdose

A

Flumazenil (competitive antagonist at GABA benzodiazepine receptor)

28
Q

Which benzodiazepine drugs are used for status epilepticus?

A

Lorazepam

Diazepam

29
Q

What drug class do these belong to?

Midazolam

Chlordiazepoxide

Alprazolam

A

Benzodiazepine

30
Q

What class of drugs are these?

Zolpidem

Zaleplon

Eszopiclone

A

Nonbenzodiazepine hypnotics

31
Q

Mechanism of Nonbenzodiazepine hypnotics

A

Act via BZ1 receptor subtype of the GABA receptor

32
Q

Clinical use of Nonbenzodiazepine hypnotics

A

insomnia

33
Q

Toxicity of Nonbenzodiazepine hypnotics

A

Ataxia

Headaches

Confusion

Short duration because of rapid metabolism by liver enzymes

Unlike older sedative-hypnotics, cause only modest-after psychomotor depression and few amnestic effects

Lower dependence risk than benzodiazepine

34
Q

What class of drugs is halothane, enflurance and isoflurane?

A

Inhaled anesthetics

35
Q

What class of drugs is methoxyflurane and nitrous oxide?

A

Inhaled anesthetic

36
Q

Mechanism of inhaled anesthetics

A

Mechanism unknown

37
Q

Effects of inhaled anesthetics

A

Myocardial depression

Respiratory depression

Nausea/emesis

Increased cerebral blood flow (decreased cerebral metabolic demand)

38
Q

Toxicity of inhaled anesthetics

A

Malignant hyperthermia (all but nitrous oxide; inherited suceptibility)

39
Q

Toxicity of halothane

A

Hepatotoxicity

40
Q

Toxicity of methoxyflurane

A

Nephrotoxicity

41
Q

Toxicity of enflurane

A

Proconvulsant

42
Q

Toxicity of nitrous oxide

A

Expansion of trapped gas in a body cavity

43
Q

What are 5 classes of IV anesthetics?

A

Barbiturates

Benzodiazepines

Arylcyclohexylamines (Ketamine)

Opioids

Propofol

“BB King on OPIOIDS PROPOses FOOLishly”

44
Q

Which barbiturate is used as an IV anesthetic and describe its kinetics?

A

Thiopental

High potency (high lipid solubility)

Rapid entry into brain

45
Q

What is the use of thiopental in IV anesthetic? How are its effects terminated

A

Used for induction of anesthesia and short surgical procedures

Effects terminated by rapid redsitribution into tissue and fat

46
Q

Which benzodiazepine is most often used for endoscopy?

A

Midazolam

47
Q

What other drugs must benzodiazepines be used with for IV anesthetic?

A

Used adjunctively with gaseous anesthetics and narcotics

48
Q

Toxicity of benzodiazepine use in IV anesthetics?

A

May cause severe post-op respiratory depression, decreased BP and amnesia

49
Q

What is ketamine a derivative of?

A

PCP analog

50
Q

What is the clinical use of ketamine?

A

Dissociative anesthetic

Cardiovascular stimulant

51
Q

Mechanism of ketamine

A

Block NMDA receptors

52
Q

Use of opioids in IV anesthetic

A

Used with other CNS depressants during general anesthesia

53
Q

What are propofol anesthetic uses?

A

Sedation in ICU

Rapid anesthesia induction

Short procedures

54
Q

Mechanism of propofol

A

Potentiates GABAA

55
Q

What are the two classes of local anesthetics?

A

Esters (procaine, cocaine, tetracaine)

Amides (amides have two I’s in their name; i.e. lidocaine, mepivacaine, etc)

56
Q

Mechanism of local anesthetics

A

Block Na channels by binding to specific receptors on inner portion of channel

Preferentially binds to activated Na channels so most effective in rapidly firing neurons

Tertiary amine local anesthetics penetrate membrane in uncharged form then bind to ion channels as charged form

57
Q

Clinical use of local anesthetics

A

Minor surgical procedures

Spinal anesthetic

58
Q

Toxicity of local anesthetics

A

CNS excitation

Severe cardiovascular toxicity (bupivacaine)

HTN

Hypotension

Arrhythmias (cocaine)

CNS Pathology (11 decks)

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