CNS Depressants Flashcards

(70 cards)

1
Q

Are CNS depressant sympatholytic or sympathomimetic

A

Sympatholytic

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2
Q

Most widely used substance of abuse

A

Alcohol

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3
Q

Medical uses of ethanol

A

Relief long lasting pain
Methyl alcohol and ethylene glycol poisoning
Disinfectant or antiseptic
Solvent

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4
Q

How is alcohol used to treat long lasting pain

A

Epidural, subarachnoid and lumbar paravertebral injections of ethanol destroys sympathetic ganglia and produce vasodilation and relieve pain

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5
Q

Which enzymes metabolize alcohol

A

Alcohol dehydrogenase
Aldehyde dehydrogenase
Mixed function microsomal oxidase (Cytochrome p450 2E1) or Microsomal Ethanol Oxidising Systems (MEOS)

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6
Q

Explain the biphasic activity of ethanol

A

Preferential suppression of inhibitory neurons followed by
Global inhibition of all CNS Neurons

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7
Q

Which receptors or pathways does alcohol affect

A

Enhance GABA and Glycine inhibition
Inhibit VG Ça channels
Activates K channels
Inhibits ionotropic Glutamate receptors
Inhibits adenosine transport

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8
Q

Effects of alcohol diuresis

A

Dehydration
Thirst
Lightheadedness

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9
Q

How does alcohol trigger an inflammatory response

A

Direct toxicity of acetaldehyde and alcohol on neurons

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10
Q

Effects of alcohol on glucose metabolism

A

Causes hypoglycemia by inhibiting gluconeogenesis

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11
Q

Effects of alcohol on vascular smooth muscle

A

Alcohol and acetaldehyde causes vasodilation

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12
Q

Effects of alcohol on gastric mucosa

A

Irritates lining of stomach and stimulates acid secretion

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13
Q

Why is acetaminophen avoided in managing alcohol abuse

A

It can exacerbate hepatotoxicity

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14
Q

Which drugs are used to alleviate acute symptoms of alcohol withdrawal

A

Benzodiazepines
Propranolol
Clonidine

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15
Q

Drugs to reduce alcohol craving

A

Naltrexone
Nalmefene
Baclofen
Acamprosate

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16
Q

Drugs to maintain remission in alcoholism

A

Topiramate
Acamprosate

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17
Q

Which fluid is used to replace potassium in hospitalized alcoholics

A

Ringers lactate

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18
Q

Which antacids are preferred to manage stomach upset in alcoholics

A

Aluminium based antacids are preferred over magnesium based antacids

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19
Q

Mild to moderate symptoms of alcohol withdrawal

A

Sweats
Tachycardia
Tremors
Insomnia
Anxiety
Psychomotor agitation

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20
Q

Severe symptoms of alcohol withdrawal

A

Generalised tonic clonic seizures
Delirium tremens
Hallucinations

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21
Q

Which receptors mediate alcohol withdrawal symptoms

A

GABA receptors
NMDA receptors

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22
Q

Which benzodiazepines are preferred in alcohol withdrawal

A

Longer acting ones
Chlordiazepoxide
Clorazepate
Diazepam

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23
Q

Why are longer acting benzodiazepines preferred in alcohol withdrawal

A

Easier weaning because they usually self taper on metabolism and excretion, leading to less fluctuations in plasma drug levels
They cause fewer rebours effects and withdrawal seizures

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24
Q

When are short acting benzodiazepines used in alcohol withdrawal

A

For alcoholics with liver disease and the elderly

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25
Examples of short acting benzodiazepines
Lorazepam Oxazepam Temazepam
26
Role of thiamine and other vitamins in managing alcoholism
To increase glucose utilization by the brain
27
Role of antipsychotics in alcoholism management
To manage hallucinations and severe agitation
28
Examples of antipsychotics used in alcohol withdrawal
Haloperidol Quetiapine
29
Role of baclofen in alcohol withdrawal
GABAb receptor agonist Skeletal muscle relaxant Antispasmodic
30
Role of clonidine in managing alcohol withdrawal
alpha 2 agonist Inhibits exaggerated neurotransmitter release
31
Role of propranolol in alcohol withdrawal
Blocks effects of excessive sympathetic activity
32
Name some agents whose metabolism is inhibited by disulfiram
Phenytoin Oral anticoagulants Isoniazid
33
Drugs that can inhibit aldehyde dehydrogenase
Metronidazole Cefotetan Trimethoprim Disulfiram
34
Why is the combination of naltrexone and disulfiram avoided
Both are hepatotoxic
35
Acamprosate is avoided in which patients
Patients with severe renal impairment
36
Common adverse effects of Acamprosate
GIT effects - nausea, vomiting, diarrhea Rash
37
Does Acamprosate participate in any drug drug interactions
No
38
Benefits of nalmefene in alcohol withdrawal
Longer duration of action No dose dependent hepatotoxicity Higher affinity for mu and kappa opioid receptors
39
Role of gabapentin in alcoholism
Treat epileptic seizures and neuropathic pain
40
Role of varenicline in alcohol withdrawal
Reduces alcohol consumption Also used for smoking cessation
41
What type of receptors are opioid receptors
GPCRs Coupled t Gi and inhibit adenylyl cyclase
42
Effect of mu receptors on dopamine
Located on inhibit GABA neurons which cause disinhibition of dopamine neurons
43
Effects of Mu receptor activation
Euphoria Dependence Analgesia Sedation Depression
44
Effect of kappa receptor activation
Expressed on and inhibit dopamine neurons causing dysphoria
45
Oral bioavailability of tramadol
High oral bioavailability Averaging 70% irrespective of food
46
Mechanism of tramadol
Low affinity to mu receptors Increases serotonin release Inhibits serotonin and noradrenaline reuptake
47
Symptoms of opioid withdrawal
Piloerection Dysphoria Lacrimation Mydriasis Restlessness Abdominal cramps
48
Uses of clonidine in opioid withdrawal
Attenuate the symptoms of anxiety, hypertension, piloerection, tachycardia and chills
49
Role of methadone in opioid withdrawal
long acting mu-opioid agonist that suppresses withdrawal symptoms and controls the craving for opioids in maintenance therapy
50
Why is methadone a good choice for opioid withdrawal
It has less likelihood of inducing withdrawal symptoms due to its long duration of action
51
Drugs used to maintain remission in opioid withdrawal
Naltrexone Nalmefene
52
Nalmefene or Naltrexone be used at least …… days after abstinence to avoid inducing acute withdrawal.
Seven
53
Advantages of Nalmefene relative to naltrexone
Longer half life No hepatotoxicity Greater oral bioavailability
54
Mechanism of action of buprenorphine
Partial mu receptor agonist
55
Role of buprenorphine in opioid use disorder
Reduces craving whiles blocking or blunting the euphoric effects of full agonist
56
How long should benzodiazepines be prescribed to avoid dependence
1-2 weeks
57
How long does it take to develop dependence when one is on benzodiazepines
3-4 weeks
58
For which effects are benzodiazepines mostly abused
Euphoric effects
59
Action of benzodiazepines
Sedatives Anxiolytic Anticonvulsant
60
Examples of ultrashort scaring benzodiazepines
Midazolam Zolpidem
61
Short acting benzodiazepines
Lorazepam Oxazepam Temazepam
62
Long acting benzodiazepines
Chlordiazepoxide Flurazepam Diazepam Clonazepam Clorazepate
63
Medium acting benzodiazepines
Alprazolam Nitrazepam
64
Symptoms of benzodiazepines withdrawal
Insomnia Restlessness, agitation, paranoia Severe headaches Manic disorders Perceptual disorders Hallucinations Seizures Sweating, muscle cramps, twitches
65
Anticonvulsants used in benzodiazepines withdrawal
Carbamazepine Pregabalin
66
Antidote for benzodiazepines withdrawal
Flumazenil
67
Symptoms of barbiturate toxicity
Respiratory depression Hypothermia Sweating Ataxia Generalised seizures Vertigo Slurred speech Altered consciousness Insomnia Anxiety Tremors
68
Effects for which benzodiazepines are abused
Euphoria Relaxation Drowsiness Disinhibition
69
Symptoms of barbiturates withdrawal
Grand mal seizures Increased temperature Shaky hands Tachycardia Tachypnea Insomnia Hyperthermia
70
Examples of barbiturates
Amobarbital- Amytal Secobarbital- Seconal Phenobarbital Butalbital Thiopental