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PDA Block 3 > PDA Block 3 Week 1 > Flashcards

PDA Block 3 Week 1 Flashcards

1
Q

What are the NT in the brain? Where are they primarily located?

A

NE: Locus coeruleus
Serotonin: Raphe Nuclei
Dopamine: Nucleus Acuumbans
GABA: Substantia Nigra and GP

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2
Q

Anti-Depressants

A 
Fluoxetine
Sertraline
Duloxetine
Bupropion
Mirtazapine
Amitriptyline
Clomipramine
Phenelzine
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3
Q

Amitriptyline

A

TC anti-depressant: Blocks reuptake of NE → compensatory downregulation of β-receptors & adenylate cyclase
De-methylated to active metabolites.
S/E: Anti-cholinergic effect
Toxicity: Arrhythmia

Used for chronic pain, depression

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4
Q

Clomipramine

A

TC anti-depressant: Blocks reuptake of NE → compensatory downregulation of β-receptors & adenylate cyclase.
S/E: Anti-cholinergic effect
Toxicity: Arrhythmia

Used for OCD

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5
Q

Fluoxetine

A

SSRI (Prozac)
Block Serotonin and NE (SERT) reuptake. Active metabolite with long half life.

Major depressive disorder, OCD, Panic disorder, social phobia, PTSD, Anxiety, PMS

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6
Q

Bupropion

A

Atypical anti-depressant
Blocks NE and dopamine uptake.
Also approved for nicotine withdrawal and seasonal affective disorder

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7
Q

Mirtazapine

A

Atypical anti-depressant
Blocks pre-synaptic alpha2 R in brain.
Increases appetite

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8
Q

Duloxetine

A

SNRI (cymbalta)
Block serotonin and NE uptake. 12-18 half life.
Used with caution in pt with liver disease.
Also approved for fibromyalgia, diabetic neuropathy, back pain

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9
Q

Phenelzine

A

MAOi- irreversible
Block oxidative deamination og biogenic amines inc. NE, DA and serotonin, and ingested amines.

Anti-depressant action takes 2 weeks. Used for major depression–Produces mood elevation in depressed patients. Drugs and food interactions (tyramine) can produce hypertensive crisis.

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10
Q

Sertraline

A

SSRI (Zoloft)
Block serotonin and NE reuptake.
Shorter half life than fluoxetine.
Used for depression, OCD, panic disorder, social phobia, OCD

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11
Q

Anti-psychotics

A 
Chlorpromazine
Thioridazine
Fluphenazine
Haloperidol
Clozapine
Olanzapine
Risperidone
Quetiapine
Aripiprazole
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12
Q

Chlorpromazine

A

Anti-psychotic

Phenothiazine with aliphatic side chain. Low to medium potency, sedative, pronounced anti-cholinergic actions

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13
Q

Clozapine

A

Atypical Anti-psychotic

less extrapyramidal symptoms. May cause agranulocytosis or blood dyscrasias. Weight gain. Effect on negative symptoms

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14
Q

Thioridazine

A

Anti-psychotic

Phenothiazine with piperidine side chain. Low potency, sedative, less extrapyramidal actions, anti-cholinergic

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15
Q

Fluphenazine

A

Anti-psychotic
Phenothiazine with piperazine side chain. High potency, less sedative, less anticholinergic, more extrapyramidal reactions

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16
Q

Haloperidol

A

Anti-psychotic

Butyrophenone derivative. High potency, less sedative, less anti-cholinergic

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17
Q

Olanzapine

A

Atypical Anti-psychotic

More potent as 5HT2 antagonist. Few extra pyramidal symptoms. No agranulocytosis. Weight gain and diabetes risk

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18
Q

Risperidone

A

Atypical Anti-psychotic

Combined dopamine and serotonin receptor antagonist. Low incidence of extrapyramidal side effects

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19
Q

Quetiapine

A

Atypical Anti-psychotic

Effects on D3 and 5HT2 receptors

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20
Q

Aripiprazole

A

D2 partial agonist

approved as adjunct in treatment of depression

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21
Q

Anti-Manic

A

Lithium
Valproic Acid
Divalproex
Carbamazepine

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22
Q

Lithium

A

Anti-Manic
MOA: phosphatase that decrease IP. Decreases second messangers. Readily absorbed after oral administration. Sodium levels affect lithium excretion. Narrow therapeutic widow. Used for manic episodes and prevent recurrences of bi-polar depression and mania
SE: Fatigue, muscular weakness, tremor, GI symptoms, goiter. Use with caution in pregnancy

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23
Q

Valproic Acid

A

Anti-seizure
MOA: blocks repetitive neuronal firing. Increases GABA concentration. PK: well absorbed orally, bound to plasma protein, inhibits metabolism of phenytoin SE: GI upset, weight gain, hair loss, idiosyncratic hepatotoxicity, teratogen

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24
Q

Divalproex

A

Anti-seizure

MOA: alters ion conduction (use depedent effect Na+), inhibits generation of repetive AP.

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25
Q

Carbamazepine

A

Anti-seizure
MOA: blocks Na channels. Used for Bipolar I disoder, acute manic episodes. PhK: unpredictable absorption, hepatic enzyme induction, toxicity is dose related Toxicity: diplopia and ataxia, GI upset, drowsiness, rare blood dyscrasias, teratogen

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26
Q

Anti-Anxiety

A

Alprazolam
Buspirone
Flumazenil

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27
Q

Hypnotic

A

Chloral Hydrate
Flurazepam
Lorazepam
Pentobarbital

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28
Q

Muscle relaxant

A

Diazepam
Baclofen
Tizanidine

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29
Q

General Anesthesia: Parental

A 
Sodium thiopental
Propofol
Etomidate
Ketamine
Midazolam
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30
Q

Sodium thiopental

A

Barbituarate.
Used to induce anesthesia parentally
Unconsciousness in 10 to 30 sec. DOA =10min. Long half life=12 hrs
SE: CNS reduces cerebral oxygen utilization–> reduces cerebral blood flow and intracranial pressure. CV: produces vasodilation ( severe drops in BP); Respiratory depression

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31
Q

Propofol

A

Anesthesia-Parental Anti-emetic (advantage).
Shorter DOA than thiopental.
SE: pain on injection. Can produce excitation during induction. CNS: reduces cerebral oxygen utilization. Blunts baroreceptor reflexes. Produces more respiratory depression.

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32
Q

Etomidate

A

Anesthesia-Parental
Primary used to induce anesthesia in patients at risk for hypotension. Only used to induce anesthesia in patients prone to heymodynamic problems SE: Adrenal supression. high incidence of pain on injection and myoclonus (pre-med). CNS: reduces cerebral blood flow; CV: less than thiopental and propofol. Less respiratory depression than thiopental. More n/v.

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33
Q

Ketamine

A

Anesthesia-Parental
Produces dissociative anestheisa. Characterized by profound analgesia, unresponsiveness to commands, amnesia, spontaneous respiration. Advantage: analgesia, little respiratory depression, bronchodilator. Reserved for pt with bronchospasm (children undergoing short, painful procedures)
SE: produces nystagmus, salivation, lacrmination, spontaneous limb movements and increased muscle tone. Increased intracranial pressure. Emergence delirium hullucinations, vivid dreams, illusions. Increased bp

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34
Q

Midazolam

A

Anesthesia-Parental
Short acting benzodiazepine. Half life 1-5 hours. Used for concious sedation, anxiolysis and amnesia during minor surgical produres. Used as an adjunct regional anesthesia. Anti-anxiety so useful for pre-op. Slower induction time and long duration than thiopental
SE: respiratory depression and respiratory arrest. Use with caution with neuromuscular disease, Parkinson’s disease. CV: vasodilation

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35
Q

Isoflurane

A

Inhaled anesthesia
99% excreted unchanged from lungs. Co-administration of nitrous oxide
SE; Resp- airway irritant. Dec. tidial vol. incr. RR. Repiratory depressant. CV: myocardial depression–> dec. BP, arrythmia, dilates cerebral bv (inc. intracranial pressure)

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36
Q

Desflurane

A

Inhaled anesthesia
Very volatile (requires special equip.) low BG co-eff. Predominantly excreted unchanged. Used for outpatient surgeries. Produces direct skeletal m. relaxation
SE: respiratory irritant

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37
Q

Sevoflurane

A

Inhaled anesthesia
Very low B:G coeff. Use: induction and maintainence in children and adults. Not a respiratory irritant
SE: CV: similar to isoflurane. Resp- similar to isoflurane, less resp depression

38
Q

Nitrous oxide

A

Inhaled anesthesia
rapid induction and recovery. Rapid uptake from alveoli results in concentration of gases that are co-administered. Can dilute O2 so need 100% O2 on emergence. 99% excretion through lungs. Used: weak anesthetic ( cannot be used at greater than 80% due to oxygen requirements) Used to produce sedation and analgesia in outpatient dentistry
SE: can exchange with nitrogen in any air-containing cavity so contraindicated in pneumothorax. Negative inotrope, but also sympatho-stimulant

39
Q

Local Anesthetic

A 
Cocaine
Procaine 
Tetracaine 
Benzocaine
Lidocaine
Bupivacaine
Ropivacaine
40
Q

Cocaine

A

Local Anesthetics- Ester Blocks NE uptake into presynaptic adrenergic nerves. Vasoconstrictor properties. Used for topical anestheisal of Upper Respiratory tract (to limit bleeding)

41
Q

Procaine

A

Local Anesthetics- Ester Short acting. Used for infiltration anesthesia. Low potenency,. Slow onset and Short DOA

42
Q

Tetracaine

A

Local Anesthetics- Ester Long acting. More potent and longer acting than procaine. Used in spinal anesthesia and topical and ophthalmic preps. Not sured for peripheral nerve block bc requires large doses

43
Q

Benzocaine

A

Local Anesthetics- Ester

Low solubility in water so absorbed slowly. Used for wounds and ulcerated surface for long relief

44
Q

Lidocaine

A

Local Anesthetic-Amide intermediate DOA, faster, more intense, longer lasting and extensive anesthesia than procaine. Use with epinephrine decreases rate of absorption –> decreases toxicity. Metabolized in liver

45
Q

Bupivacaine

A

Local Anesthetic-Amide
Long acting, can produce prolonged anesthesia. Long DOA. More cardiotoxic than lidocaine. S-enantiomer is available that is less cardiotoxic

46
Q

Ropivacaine

A

Local Anesthetic-Amide S-enantiomer. Less cardiotoxicity than bupivacaine, but similar action. Used for epidural and region anesthesia. More motor sparing

47
Q

Ethanol

A

Small water soluble molecule that is absorbed rapidly from GI tract after oral administration (small SI). Rate of absorption influenced by ethanol concentration (carbon dioxide–>decreased if gastric emptying is delayed)- Distributed to total body water. Significant first past effect

48
Q

Alcohol dehydrogenase

A

primary pathway for ethanol oxidation to acetaldehyde= rate limiting (liver). First order at single dose ( 10g/hr in 70g person)

49
Q

Microsomal Ethanol Oxidizing System

A

Mixed function oxidase system. High Km- little contribution at concentrations below 100 mg/dl. Induced in alcoholics (CYP 2E1)

50
Q

Disulfiram

A

inhibits aldehyde dehydrogenase (ALDH). Aversion therapy. Pharm effect: Acetaldehyde syndrome

51
Q

Benzodiazepines

A

Diazepam– gradual reduction of dose “tapering off”

52
Q

Chlordiazepoxide

A

Benzodiazepine for management of alcohol withdrawal syndrome. Prevention of seizures, delirium

53
Q

Diazepam

A

Benzodiazepine for management of alcohol withdrawal syndrome. Prevention of seizures, delirium

54
Q

Naltrexone

A

Use: reduces the urge to drink in alcohol withdrawal. MOA= opioid receptor antagonist.

55
Q

Acamprosate

A

Decreases drinking frequency and reduces relapse. MOA: GABA mimetic. Well tolerated- primary side effect is diarrhea

56
Q

CNS stimulants

A 
Caffeine
Adenosine
Methylphenidate
Cocaine
Amphetamine
Methamphetamine
Nicotine
Bupropion
Varenicline
57
Q

Caffeine

A

methylxanthine compound found in coffee. One cup of coffee can have 80-200 mg of caffeine
MOA: blocks adenosine reeptors thought to be mechanism for CNS stimulation. Postsynaptic adenosine receptors produce IPSP. Presynaptic adenosine reeptors inhibit glutamate release. Caffeine blocks both of these inhibitor effects–> CNS stimulation. Inhibitions of phosphodiesterase–> increases cAMP concentration. Induces release of calcium from intracellular stores (ER) use: aid to stay awake, treatment of headache.
Toxicity: excessive CNS stimulation, nervousness, insomnia, excitement. Chronic use: Tolerance developed to stimulant effects of caffeine. Physical dependence develops at a dose of 2 cups of coffee a day

58
Q

Adenosine

A

Postsynaptic adenosine receptors produce IPSP. Presynaptic adenosine receptors inhibit glutamate release.

59
Q

Methylphenidate

A

Structurally similar to Amphetamine

- Used for Narcolepsy & ADD

60
Q

Alcohol Pharmacology

A

Naltrexone: reduce urge to drink

i. Increases control
ii. MOA: opioid receptor antagonist→ reduces craving
iii. Psychosocial therapy-10 step program

Acamprosate: decreases drinking frequency and reduces relapse

i. MOA: GABAa mimetic
ii. Normalize disregulated transmission
iii. SE: diarrhea

Disulfiram: aversion therapy

i. MOA: inhibition of aldehyde dehydrogenase
ii. Pharm effects: acetaldehyde syndrome
iii. Not very effective—ethnical issues (requires considerable will power)

61
Q

Cocaine

A

Sympathomimetic Stimulants: psychoactive alkaloid
Weak base, unprotonated form is unionized–> predominant alkaline pH. PharmK: well absorbed through mucous membranes. Shorter for IV and smoked than oral. Metabolized by serum and liver esterases. Short half life potent inhibitor of the reuptake of noreepinephrine, dopamine and serotonin. Increases typrosine and tryptophan hydroxylase (loss of inhibition).
Causes: vasoconstriction, tachycardia (sympathomimetic), increased alertness.
Use: local anesthesia in upper Respiratory tract

62
Q

Amphetamine

A

Sympathomimetic stimulant Well absorbed orally. Longer duration 4-6 hours
Releases NE, dopamine and serotonin. Blocks transmitter uptake into pre-synaptic terminals. Direct partial alpha adrenergic receptors.
Causes: wakefullness, alertness, decreased fatigue, respiratory stimulation, decrase appetite.
Peripheral sympathomimetic. Used for narcolepsy and ADD

63
Q

Methamphetamine

A

More CNS effect than Amphetamine. (Narcolepsy and ADD)

64
Q

Amphetamine & Amphetamine like

A

Amphetamine
Methamphetamine
Methylphenidate

SE: insomnia, abdominal pain, anorexia, suppression of growth, fever, facial tics
Toxicity:
Acute: sympathomimetic, - restlessness, dizziness
- Psychosis
- Neurotoxicity—can lead to permanent intellectual problems
- Meth mouth: severe tooth decay, dry mouth+ increased sugary drinks

65
Q

Nicotine

A

Sympathomimetic stimulant Agonist of nicotinic cholinergic receptors.
Absorbed readily. Tolerance occurs throughout the day Sympathetic ganglia activation–> release of NE. PS ganglia activity results in GI effects (nausea, increased motility).
CNS effects: activates dopamine signaling–> reinforcement. Muscle relaxant

66
Q

Bupropion

A

Ncotine replacement therapy unknown MOA, seems to enhance NE and dopamine signaling Reduces cravings and nicotine withdrawal symptoms

67
Q

Varenicline

A

Partial agonist of CNS nicotinic receptors

- activates nicotinic receptors to reduce craving and withdrawal. Reduces effects of full agonist

68
Q

Opioid Receptor Agonists

A 
Morphine
Fentanyl
Meperidine
Methadone
Heroin
Codeine
Oxycodone
Hydrocodone
Hydromorphone
69
Q

Endogenous Opioid R Agonist

A

Β- Endorphin
Dynorphin
Enkephalin

70
Q

Opioid R Agonist/Antagonist

A

Nalbuphine

Buprenorphine

71
Q

Drugs Related to opioids

A

Dextromethorphan
Tramadol
Suboxone

72
Q

Morphine

A

Mu R agonist

MS Contin. Analgesic. Low oral to parental potency 3:1. Duration: 4-5 hours

73
Q

Fentanyl

A

Mu R agonist
structurally related to Meperidine. 100x as potent as morphine. Short acting. Injectable and transdermal and as buccal film for breakthrough pain

74
Q

Meperidine

A

Mu R agonist

Shorter DOA of analgesia than morphine. Forms toxic metabolite that can accumulate. Interactions with MAO inhibitors

75
Q

Methadone

A

Mu R agonist

equipotent with morphine. Good oral availability. Long DOA. Used in treatment of opiod abuse and chronic pain

76
Q

Heroin

A

Mu R agonist

diacetyl morphine. More lipophilic than morphone. Converted to 6-mono acetyl morphine and morphone. High abuse potential

77
Q

Codeine

A

Mu R agonist

O-methyl morphone- mild to moderate pain. Some codeine is metabolized to morphine

78
Q

Oxycodone

A

Mu R agonist

Oxycotin- moderate to severe pain. Major abuse problem

79
Q

Hydrocodone

A

Mu R agonist

Vicodin-moderate to severe pain

80
Q

Hydromorphone

A

Mu R agonist

2-3x as potent as morphine

81
Q

Nalbuphine

A

mu antagonist and kappa agonists

- similar in efficacy and potency as morphine. Much lower abuse potential. Injectable form only

82
Q

Buprenorphine

A

partial mu agonist
used to treat moderate to severe pain.
Buprenorphone + naloxone is used to treat opioid dependence

83
Q

Naloxone

A
  • opioid antagonist
  • high affinity for mu receptors. Short DOA 1-2 hours. Used to treat opioid OD. Can be combined with opioids to decrease parental abuse liability
84
Q

Naltrexone

A
  • opioid antagonist

orally active with long half life. Can be used in treatment of alcoholism and opiate addiction

85
Q

Β- Endorphin

A

Endogenous ligand of mu receptor Gi–> decrease adenylate cyclase–> decrease cAMP–> increase K+–> decrease in Ca–> decrease in NT release

86
Q

Dynorphin

A

endogenous ligand of kappa receptor Gi–> decrease adenylate cyclase–> decrease cAMP–> decrease in Ca–> decrease in NT release

87
Q

Enkephalin

A

Endodogenous ligand of delta receptor Gi–> decrease adenylate cyclase–> decrease cAMP–> increase K+–> decrease in Ca–> decrease in NT release

88
Q

Dextromethorphan

A

(Robitussin) Antitussive not analgesic. NMDA antagonist

89
Q

Tramadol

A

(Ultram) weak mu agonist. Also blocks NE and 5HT uptake. Used for mild to moderate pain

90
Q

Suboxone

A

treatment of opioid abuse

91
Q

General Anesthesia: Inhaled

A

Isoflurane
Desflurane
Sevoflurane
Nitrous oxide

PDA Block 3 (4 decks)

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