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PDA Block 3 > PDA Block 3 Week 1 > Flashcards

PDA Block 3 Week 1 Flashcards

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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
Carbamazepine
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
26
Anti-Anxiety
Alprazolam Buspirone Flumazenil
27
Hypnotic
Chloral Hydrate Flurazepam Lorazepam Pentobarbital
28
Muscle relaxant
Diazepam Baclofen Tizanidine
29
General Anesthesia: Parental
``` Sodium thiopental Propofol Etomidate Ketamine Midazolam ```
30
Sodium thiopental
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
31
Propofol
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.
32
Etomidate
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.
33
Ketamine
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
34
Midazolam
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
35
Isoflurane
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)
36
Desflurane
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
37
Sevoflurane
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
Nitrous oxide
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
Local Anesthetic
``` Cocaine Procaine Tetracaine Benzocaine Lidocaine Bupivacaine Ropivacaine ```
40
Cocaine
Local Anesthetics- Ester Blocks NE uptake into presynaptic adrenergic nerves. Vasoconstrictor properties. Used for topical anestheisal of Upper Respiratory tract (to limit bleeding)
41
Procaine
Local Anesthetics- Ester Short acting. Used for infiltration anesthesia. Low potenency,. Slow onset and Short DOA
42
Tetracaine
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
Benzocaine
Local Anesthetics- Ester | Low solubility in water so absorbed slowly. Used for wounds and ulcerated surface for long relief
44
Lidocaine
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
Bupivacaine
Local Anesthetic-Amide Long acting, can produce prolonged anesthesia. Long DOA. More cardiotoxic than lidocaine. S-enantiomer is available that is less cardiotoxic
46
Ropivacaine
Local Anesthetic-Amide S-enantiomer. Less cardiotoxicity than bupivacaine, but similar action. Used for epidural and region anesthesia. More motor sparing
47
Ethanol
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
Alcohol dehydrogenase
primary pathway for ethanol oxidation to acetaldehyde= rate limiting (liver). First order at single dose ( 10g/hr in 70g person)
49
Microsomal Ethanol Oxidizing System
Mixed function oxidase system. High Km- little contribution at concentrations below 100 mg/dl. Induced in alcoholics (CYP 2E1)
50
Disulfiram
inhibits aldehyde dehydrogenase (ALDH). Aversion therapy. Pharm effect: Acetaldehyde syndrome
51
Benzodiazepines
Diazepam-- gradual reduction of dose "tapering off"
52
Chlordiazepoxide
Benzodiazepine for management of alcohol withdrawal syndrome. Prevention of seizures, delirium
53
Diazepam
Benzodiazepine for management of alcohol withdrawal syndrome. Prevention of seizures, delirium
54
Naltrexone
Use: reduces the urge to drink in alcohol withdrawal. MOA= opioid receptor antagonist.
55
Acamprosate
Decreases drinking frequency and reduces relapse. MOA: GABA mimetic. Well tolerated- primary side effect is diarrhea
56
CNS stimulants
``` Caffeine Adenosine Methylphenidate Cocaine Amphetamine Methamphetamine Nicotine Bupropion Varenicline ```
57
Caffeine
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
Adenosine
Postsynaptic adenosine receptors produce IPSP. Presynaptic adenosine receptors inhibit glutamate release.
59
Methylphenidate
Structurally similar to Amphetamine | - Used for Narcolepsy & ADD
60
Alcohol Pharmacology
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
Cocaine
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
Amphetamine
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
Methamphetamine
More CNS effect than Amphetamine. (Narcolepsy and ADD)
64
Amphetamine & Amphetamine like
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
Nicotine
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
Bupropion
Ncotine replacement therapy unknown MOA, seems to enhance NE and dopamine signaling Reduces cravings and nicotine withdrawal symptoms
67
Varenicline
Partial agonist of CNS nicotinic receptors | - activates nicotinic receptors to reduce craving and withdrawal. Reduces effects of full agonist
68
Opioid Receptor Agonists
``` Morphine Fentanyl Meperidine Methadone Heroin Codeine Oxycodone Hydrocodone Hydromorphone ```
69
Endogenous Opioid R Agonist
Β- Endorphin Dynorphin Enkephalin
70
Opioid R Agonist/Antagonist
Nalbuphine | Buprenorphine
71
Drugs Related to opioids
Dextromethorphan Tramadol Suboxone
72
Morphine
Mu R agonist | MS Contin. Analgesic. Low oral to parental potency 3:1. Duration: 4-5 hours
73
Fentanyl
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
Meperidine
Mu R agonist | Shorter DOA of analgesia than morphine. Forms toxic metabolite that can accumulate. Interactions with MAO inhibitors
75
Methadone
Mu R agonist | equipotent with morphine. Good oral availability. Long DOA. Used in treatment of opiod abuse and chronic pain
76
Heroin
Mu R agonist | diacetyl morphine. More lipophilic than morphone. Converted to 6-mono acetyl morphine and morphone. High abuse potential
77
Codeine
Mu R agonist | O-methyl morphone- mild to moderate pain. Some codeine is metabolized to morphine
78
Oxycodone
Mu R agonist | Oxycotin- moderate to severe pain. Major abuse problem
79
Hydrocodone
Mu R agonist | Vicodin-moderate to severe pain
80
Hydromorphone
Mu R agonist | 2-3x as potent as morphine
81
Nalbuphine
mu antagonist and kappa agonists | - similar in efficacy and potency as morphine. Much lower abuse potential. Injectable form only
82
Buprenorphine
partial mu agonist used to treat moderate to severe pain. Buprenorphone + naloxone is used to treat opioid dependence
83
Naloxone
- 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
Naltrexone
- opioid antagonist | orally active with long half life. Can be used in treatment of alcoholism and opiate addiction
85
Β- Endorphin
Endogenous ligand of mu receptor Gi--> decrease adenylate cyclase--> decrease cAMP--> increase K+--> decrease in Ca--> decrease in NT release
86
Dynorphin
endogenous ligand of kappa receptor Gi--> decrease adenylate cyclase--> decrease cAMP--> decrease in Ca--> decrease in NT release
87
Enkephalin
Endodogenous ligand of delta receptor Gi--> decrease adenylate cyclase--> decrease cAMP--> increase K+--> decrease in Ca--> decrease in NT release
88
Dextromethorphan
(Robitussin) Antitussive not analgesic. NMDA antagonist
89
Tramadol
(Ultram) weak mu agonist. Also blocks NE and 5HT uptake. Used for mild to moderate pain
90
Suboxone
treatment of opioid abuse
91
General Anesthesia: Inhaled
Isoflurane Desflurane Sevoflurane Nitrous oxide

PDA Block 3 (4 decks)

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