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Drugs Flashcards

1
Q

Lidocaine

A
  • local anaesthetic
  • amide
  • blockade of voltage gated sodium channels, use dependent, medium acting
  • systemic doses can result in death due to the blockade of respiration, cardiovascular problems and depress smooth muscle contraction, seizures
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2
Q

Bupivacaine

A
  • local anaesthetic
  • blockade of voltage gated sodium channels, use dependent, long acting
  • systemic doses can result in death due to the blockade of respiration, cardiovascular problems and depress smooth muscle contraction, seizures
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3
Q

Procaine

A
  • local anaesthetic
  • ester - can cause a local allergic reaction via a para-aminobenzoic acid (PABA) formation
  • blockade of voltage gated sodium channels, use dependent, short acting
  • systemic doses can result in death due to the blockade of respiration, cardiovascular problems and depress smooth muscle contraction, seizures.
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4
Q

Benzocaine

A
  • local anasthetic
  • ester - can cause a local allergic reaction via a para-aminobenzoic acid (PABA) formation
  • blockade of voltage gated sodium channels, surface use only and lacks efficacy, short acting
  • systemic doses can result in death due to the blockade of respiration, cardiovascular problems and depress smooth muscle contraction, seizures.
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5
Q

Cocaine

A
  • local anaesthetic
  • ester - can cause a local allergic reaction via a para-aminobenzoic acid (PABA) formation
  • blockade of voltage gated sodium channels, in addition, due to cocaine’s ability to block reputable of NE, an also result in local vasoconstriction, medium acting.
  • systemic doses can result in death due to the blockade of respiration, cardiovascular problems and depress smooth muscle contraction, seizures, also can lead to addiction due to its ability to block reuptake of dopamine
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6
Q

Pancuronium

A
  • neuromuscular blocker
  • competitive agent
  • skeletal muscle nicotinic channel antagonist, long duration of action (ie 60 minutes)
  • ganglionic blockade causing decrease in blood pressure and tachycardia, release of histamine, respiratory paralysis
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7
Q

Atracurium

A
  • neuromuscular blocker
  • competitive agents
  • skeletal muscle nicotinic channel antagonist, intermediate duration of action
  • ganglionic blockade causing decrease in blood reassure and tachycardia, release of histamine, respiratory paralysis
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8
Q

Vecuronium

A
  • neuromuscular blocker
  • competitive agents
  • skeletal muscle nicotinic channel antagonist, intermediate duration of action
  • ganglionic blockade causing decrease in blood reassure and tachycardia, release of histamine, respiratory paralysis
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9
Q

Succinylcholine

A
  • neuromuscular blocker
  • depolarising agent
  • skeletal muscle nicotinic channel agonist, metabolised by butyrylcholinesterase, not metabolised by acetylcholinesterase so the channels cannot “reset” and myocyte cannot depolarise
  • can cause MALIGNANT HYPERTHERMIA, high body temperature, tachycardia, bradycardia, release of histamine, rigid muscles, muscle breakdown and respiratory paralysis
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10
Q

Dantrolene

A
  • spasmolytic
  • used for malignant hypothermia and ALS
  • blocks calcium release from the sarcoplastic reticulum by blocking the ryanodine receptor
  • dizziness, drowsiness, weakness, fatigue, GI disturbances, respiratory depression
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11
Q

Diazepam

A
  • spasmolytic and anti-anxiety
  • long acting benzodiazepine
  • potentiate GABAs ability to open GABA A chloride channel (increase channel opening frequency
  • sedation, ataxia, dependence
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12
Q

Baclofen

A
  • spasmolytics
  • GABA B agonist (GPCR inhibitory coupling)
  • dizziness, drowsiness, weakness, fatigue, seizures, hallucinations
  • ALS
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13
Q

Botulinum Toxin

A
  • spasmolytic
  • inhibits release of acetylcholine at the NMJ
  • anxiety, dizziness, drowsiness, dry eyes and mouth, back and neck pain
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14
Q

Carisoprodol

A
  • spasmolytic
  • potentiate GABAs ability to open the GABA A chloride channel (increase channel opening frequency
  • sedation, ataxia, somnolence, dependence, withdrawal
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15
Q

Morphine

A
  • opioid
  • acts at my GPCR to cause opening K+ channels and blocks VGCC
  • constipation, respiratory depression, abuse potential
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16
Q

Codeine

A
  • opioid
  • acts at my GPCR to cause opening K+ channels and blocks VGCC, less potent than morphine, better bioavailability
  • constipation, respiratory depression, abuse potential
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17
Q

Oxycodone

A

•opioid
•acts at my GPCR to cause opening K+ channels and blocks VGCC
-percocet contains acetaminophen
-percodan contains aspirin
•constipation, respiratory depression, abuse potential

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18
Q

Fentanyl

A
  • opioid
  • acts at my GPCR to cause opening K+ channels and blocks VGCC, my anatgonist, 100 times more potent than morphine
  • constipation, respiratory depression, abuse potential
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19
Q

Methadone

A
  • opioid
  • acts at my GPCR to cause opening K+ channels and blocks VGCC, orally available mu opioid agonist
  • constipation, respiratory depression, abuse potential
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20
Q

Loperamide

A
  • opioid
  • acts at my GPCR to cause opening K+ channels and blocks VGCC, weak (less potent) mu agonist that does not cross the blood brain barrier, used for diarrhea
  • severe constipation
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21
Q

Buprenorphine

A
  • opioid
  • partial mu agonist and Kappa opioid agonist/antagonist
  • acts at my GPCR to cause opening K+ channels and blocks VGCC
  • constipation, respiratory depression, abuse potential, dysphoria and opioid withdrawal
  • +naloxone - used to order to reduce opioid use and abuse, an opioid receptor agonist
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22
Q

Tramadol

A
  • opioids
  • partial mu agonist and Kappa opioid agonist/antagonist
  • acts at my GPCR to cause opening K+ channels and blocks VGCC, weak mu agonist, also inhibits uptake of NE and 5HT
  • severe constipation, some dysphoria and opioid withdrawal, less abuse potential
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23
Q

Naloxone

A
  • not for pain but used for opioid overdose, opioid antagonist
  • blocks opioid receptors, short acting (30-90 minutes)
  • will cause immediate withdrawal symptoms in opioid addiction
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24
Q

Naltrexone

A
  • not for pain but used for opioid overdose, opioid antagonist
  • blocks opioid receptors, longer acting (4-14 hrs)
  • will cause immediate withdrawal symptoms in opioid addiction
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25
Q

Aspirin

A
  • NSAID
  • many acetyl and non acetyl salicylates available
  • irreversible COX inhibition
  • GI irritation, GERD and GI ulcers, Reye Syndrome in children (aspirin only)
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26
Q

Ibuprofen

A
  • NSAID
  • reversible COX inhibition
  • GI irritation, GERD and GI ulcers
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27
Q

Indomethacin

A
  • NSAID
  • ductus arteriosus
  • reversible COX inhibition
  • GI irritation, GERD and GI ulcers
  • contraindicated with Lithium
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28
Q

Ketoprofen

A
  • NSAID
  • ductus arteriosus
  • reversible COX inhibition
  • GI irritation, GERD and GI ulcers
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29
Q

Naproxen

A
  • NSAID
  • ductus arteriosus
  • reversible COX inhibition
  • GI irritation, GERD and GI ulcers
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30
Q

Celecoxib

A
  • NSAID
  • considered irreversible COX2 inhibition, reversible COX1 inhibition
  • lacks GI effects, can cause cardiovascular problems, including stroke and myocardial infarction, can decrease kidney function
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31
Q

Acetaminophen

A
  • pain medication
  • paracetamol
  • thought to inhibit some COX enzyme, other mechanism unknown
  • can be hepatotoxic, skin rash, contraindicated in alcoholism
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32
Q

Dexamethasone

A
  • glucocorticoid
  • increase levels of lipocortin (also known as Annexin), that inhibits phospholipids A2, decreasing inflammatory mediators, nuclear receptor-altering gene expression (oral)
  • immunosuppression
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33
Q

Prednisone

A
  • glucocorticoid
  • increase levels of lipocortin (also known as Annexin), that inhibits phospholipids A2, decreasing inflammatory mediators, nuclear receptor-altering gene expression (oral)
  • immunosuppression
  • myasthenia gravis for immunosupression and cushingoid
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34
Q

Hydrocortisone

A
  • glucocorticoid
  • increase levels of lipocortin (also known as Annexin), that inhibits phospholipids A2, decreasing inflammatory mediators, nuclear receptor-altering gene expression (topical)
  • immunosuppression
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35
Q

Gabapentin

A
  • chronic pain
  • A2∂ ligand
  • decrease the number of voltage sensitive calcium channels on membrane surface
  • sedation, somnolence, dizziness, ataxia, peripheral edema
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36
Q

Pregabalin

A
  • chronic pain
  • A2∂ ligand
  • decrease the number of voltage sensitive calcium channels on membrane surface
  • sedation, somnolence, dizziness, ataxia, peripheral edema, visual disturbances
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37
Q

Amitriptyline
Nortriptyline
Desipramine

A
  • chronic pain
  • tricyclic antidepressants (TCAs), increase levels of NE and 5HT
  • norepinephrine and serotonin reuptake inhibitors
  • antimuscarinic action
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38
Q

Duloxetine

A
  • chronic pain
  • serotonin and norepinephrine reuptake inhibitors (SNRIs)
  • norepinephrine and serotonin reuptake inhibitors
  • hypertension, sexual and GI disturbances, somnolence, dizziness
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39
Q

Lidocaine

A
  • chronic pain
  • blocks voltage gated sodium channels
  • patch
  • if high systemic doses are reached can cause cardiovascular arrythmia, seizures
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40
Q

Carbamazepine

A
  • chronic pain, mood stabilizer
  • inactivation of VGNa+ channels
  • prolong fast inactivation of voltage gated sodium channels
  • teratogenic, SJS, TEN, motor coordination
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41
Q

Lamotrigine

A
  • chronic pain, mood stabilizer
  • inactivation of VGNa+ channels
  • prolong fast inactivation of voltage gated sodium channels in addition may block some glutamate release and calcium channels
  • insomnia, SJS, TENs
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42
Q

Clonidine

A
  • chronic pain
  • inactivation of VGNa+ channels
  • agonist at NE-alpha2, inhibits release of pain neurotransmitters
  • hypotension
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43
Q

Sumatriptan

A
  • migraine
  • triptans “serotonin agonists”
  • 5HTIB and 5HTID agonist
  • cardiovascular, coronary artery vasospasm, contraindicated in individuals with previous MI
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44
Q

Rizatripan

A
  • migraine
  • triptans “serotonin agonists”
  • 5HTIB and 5HTID agonist
  • cardiovascular, coronary artery vasospasm, contraindicated in individuals with previous MI
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45
Q

Naratriptan

A
  • migraine
  • triptans “serotonin agonists”
  • 5HTIB and 5HTID agonist, longest acting of the triptans (1/2 life 6 hours)
  • cardiovascular, coronary artery vasospasm, contraindicated in individuals with previous MI
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46
Q

Galcanezumab

A
  • migraine
  • CGRP antagonist
  • human monoclonal antibody that binds up CGRP (calcitonin gene related peptide)
  • injection site hypersensitivity reaction, allergic reaction
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47
Q

Fremanezumab

A
  • migraine
  • CGRP antagonist
  • human monoclonal antibody that binds up CGRP (calcitonin gene related peptide)
  • injection site hypersensitivity reaction, allergic reaction
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48
Q

Erenumab

A
  • migraine
  • CGRP antagonist
  • human monoclonal antibody that binds up CGRPR (calcitonin gene related peptide receptor)
  • injection site hypersensitivity reaction, GI issues
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49
Q

Timolol

A
  • ocular hypertension
  • decrease synthesis
  • beta 2 receptor antagonist (inhibit aqueous humour secretion)
  • bronchospasm, bradycardia
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50
Q

Apraclonidine

A
  • ocular hypertension
  • decrease synthesis
  • alpha 2 receptor agonist (inhibit aqueous humour secretion)
  • ocular allergy
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51
Q

Acetazolamide

A
  • ocular hypertension
  • decrease synthesis
  • carbonic anhydrase inhibitor (inhibit aqueous humour secretion)
  • malaise, fatigue, weight loss, anorexia, depression
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52
Q

Pilocarpine

A
  • ocular hypertension
  • increase outflow
  • cholinergic agonist
  • accommodation, miosis
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53
Q

Latanoprost

A
  • ocular hypertension
  • increase outflow
  • prostaglandin FP receptor agonist inhibitor (promotes contraction of ciliary muscle which stretches open trabecular outflow pathway)
  • eyelash growth, iridium pigmentation, conjunctival hyperemia
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54
Q

Atropine

Scopolamine

A
  • mydriasis
  • muscarinic antagonist (inhibit contraction of circular muscle, iris sphincter)
  • photosensitivity, blurred vision
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55
Q

Proparacaine

A
  • corneal anaesthesia
  • sodium channel blocker (decrease excitability of sensory nerves in corneal)
  • corneal irritation
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56
Q

Opioids

A
  • act at GPCRs through G alpha —> decrease in cAMP and protein kinase A
  • G beta gamma —> blocking VGCC and opening K+ channels = hyperpolarization
  • activate a descending pain inhibitory pathway in areas of the brainstem (disinhibition)
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57
Q

NSAIDs

A

•COX1 and COX2 inhibitors

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58
Q

Steroidal antiinflammatory medications (glucocorticoid-steroids)

A

•bind to cytosolic steroid receptors which translocations into the cell nuclei to exter its effects on glucocorticoid-responsive genes resulting in the increase ina peptide called lipocortin which inhibits phospholipase A2, an enzyme responsible for mobilising arachidonic acid from cell membranes after injury

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59
Q

Norepinephrine and/or dual reuptake inhibitors

A
  • block reuptake of serotonin or NE
  • thought to work via an increase in descending inhibition, increasing NE and 5HT in the dorsal horn of the SC to inhibit pain
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60
Q

VGSC blockers

A
  • block VGSC on all neurons

* given locally

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61
Q

Triptans

A

•agonists at 5HT receptors - found on both blood vessels and on neurons with an ability to cause vasoconstriction, reducing inflammatory and pain mediator release as well as though to decrease peripheral neuronal activity —> decrease in headache severity

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62
Q

Beta blockers

A
  • prophylactic use for migraines
  • block beta adregenic receptors reducing the ability of endogenous NE and epinephrine to act at the beta receptors resulting in a decrease in hypertension and wide spread decrease in sympathetic activity
  • full mechanism as migraine prophylactic unknown
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63
Q

CGRP inhibitors

A
  • monoclonal antibodies directed against calcitonin related polypeptides (cluster headaches) fully human
  • or calcitonin gene raelated peptide receptors (CGRPR) (migraines)humanised
64
Q

Hydrocodone

A
  • opioid
  • in Vicodin, which contains acetaminophen
  • acts at muGPCR to cause opening of K+ channels and blocks VGCC
  • constipation, decreased respiratory drive, abuse potential
65
Q

Tapentadol

A
  • opioid
  • partial mu agonist and Kappa opioid receptor agonist/antagonist, acts at muGPCR to cause opening of K+ channels an blocks VGCC
  • also inhibits uptake of NE and 5HT
  • constipation, decreased respiratory drive, abuse potential
66
Q

Physostigmine

A
  • increase outflow
  • acetylcholinesterase inhibitor (promotes contraction of ciliary muscle which stretches open trabecular outflow pathway)
  • accommodation, miosis (dimmed vision)
67
Q

Scopolamine

A
  • mydriasis
  • muscarinic antagonist (inhibit contraction of circular muscle, iris sphincter)
  • photosensitivity, blurred vision
68
Q

Phenytoin

A
  • epilepsy, partial and secondarily generalised tonic clinic seizures
  • inactivation of Na+ channels, prolongs fast inactivation of VGSC
  • teratogen, induces CYP3A4 and CYP2C9
69
Q

Topiramate

A
  • epilepsy, partial and primary generalised seizures, as well as refractory and partial and refractory generalised tonic-clonic seizures and tonic-clonic in LG
  • inactivation of Na+ channels, prolongs fast inactivation of VGSC in addition activates hyperpolarizing K+ currents, increase activity of GABAa Cl- channels, some inhibition of glutamate AMPA-kainate channels and carbonic anhydrase inhibitor
  • teratogen, inhibits CYP2C19
70
Q

Lacosamide

A
  • epilepsy, partial and secondarily generalised seizures tonic-clonic
  • inactivation of Na+ channels, prolong slow inactivation of VGSC
  • GI disturbances
71
Q

Valproic Acid

A
  • epilepsy, myoclonic, partial and tonic-clonic seizures; absence seizures, mood stabilizer
  • inactivation Na+ channels, prolong fast inactivation of VGSC, increase at GABAa Cl- channels, reduce T-type Ca2+ channel activity
  • teratogen, inhibits CYP2C9 and glucuronidation
72
Q

Zonisamide

A
  • epilepsy, partial and secondarily generalised seizures tonic-clonic and absence
  • inactivation of Na+ channels, prolongs fast inactivation of VGSC, increase GABAaCl- channels, reduce T-type Ca2+ channel activity and carbonic anhydrase inhibitor
  • somnolence
73
Q

Clonazepam

A
  • epilepsy, generalised seizures, anti-anxiety
  • long acting benzodiazepine
  • inactivation of Na+ channels, enhanced GABA synaptic transmission, benzodiazepines
  • sedation
74
Q

Clobazam

A
  • epilepsy, approved for LGS but works for all seizure types
  • inactivation of Na+ channels, potentiate GABAs ability to open the GABAaCl- channel (increase channel opening frequency)
  • sedation (but less than clonazepam)
75
Q

Pentobarbital

A
  • epilepsy, generalised seizures
  • barbiturate
  • inactivation of Na+ channels, potentiate GABA’s ability to increase duration of GABAaCl- channel openings, at high concentrations can open directly
  • sedation, respiratory depression
76
Q

Vigabatrin

A
  • epilepsy
  • inactivation of Na+ channels, inhibits the breakdown of GABA
  • somnolence
77
Q

Ethosuximide

A
  • epilepsy, absence seizures
  • voltage gated Ca2+ channel antagonist, reducing current through T-type Ca2+ channels
  • sedation
78
Q

Levetiracetam

A
  • epilepsy, adjunct therapy for myoclonic, partial onset and primary generalised seizures in adults and children
  • inhibits vesicular release, binds a protein (SV2A) on vesicles and inhibits their release. Overlay decrease in NT release
  • asthenia (weakness)
79
Q

Felbamate

A
  • epilepsy
  • glutamate NMDA channel antagonist, blocks the open state of the NMDA channels
  • aplastic anemia, liver failure
80
Q

Perampanel

A
  • epilepsy
  • AMPA receptor antagonist, non competitive binding to AMPA receptor
  • psychosis
81
Q

Carbidopa/Levodopa

A
  • Parkinson’s Disease
  • dopamine precursors, Levodopa is decarboxylase to form dopamine in the CNS; Carbidopa is added to the levodopa since it inhibits the breakdown by enzymes in he GI tract (carbidopa cannot cross the BBB)
  • dyskinesias (excessive and involuntary movements)
82
Q

Bromocriptine

A
  • Parkinson’s Disease
  • dopamine agonist, dopamine D2 receptor agonist and D1 partial agonist
  • hallucinations and confusion
83
Q

Ropinorole

A
  • Parkinson’s Disease
  • dopamine agonist, dopamine D2 and D3 receptor agonist
  • sleep disturbances
84
Q

Pramipexole

A
  • Parkinson’s Disease
  • dopamine agonist, D2 and D3 receptor agonist
  • sleep disturbances
85
Q

Amantadine

A
  • Parkinson’s Disease
  • dopamine agonist, increases dopamine release and blocks dopamine reuptake; also is a weak NMDA antagonist
  • ataxia
86
Q

Tolcapone

A
  • Parkinson’s Disease
  • COMT inhibitors, inhibitors of catechol-O-methyltransferase, inhibits dopamine breakdown
  • GI disturbances, liver toxicity
87
Q

Selegiline

A
  • Parkinson’s Disease
  • MAO inhibitors, inhibitor of monoamine oxidase B isoenzyme, inhibits dopamine breakdown in striatum
  • sedation, hypotension, serotonin syndrome
88
Q

Benztropine mesylate

A
  • Parkinson’s Disease
  • muscarinic antagonist, blocks muscarinic receptors
  • drowsiness and dizziness, blurred vision
89
Q

Trihexyphenidyl

A
  • Parkinson’s Disease
  • muscarinic antagonist, blocks muscarinic receptors
  • drowsiness and dizziness, blurred vision
90
Q

Riluzole

A
  • Amylotrophic Lateral Sclerosis (ALS)
  • diminish neuroexcitotoxicity, inhibits glutamate release by blocking VGSC, antagonist at NMDA and Kainate-type glutamate receptors
  • GI disturbances
91
Q

Riluzole

A
  • Amylotrophic Lateral Sclerosis (ALS)
  • diminish neuroexcitotoxicity, antioxidant (unknown mechanism)
  • bruising, gait disturbances
92
Q

Neostigmine

A
  • myasthenia gravis
  • cholinergic enhancers, acetylcholinterase inhibitors (reversible AChE inhibitors), tend not to cross BBB
  • GI disturbances, “SLUDGE”
93
Q

Edrophonium

A
  • myasthenia gravis
  • cholinergic enhancers, acetylcholinterase inhibitors (reversible AChE inhibitors), tend not to cross BBB
  • GI disturbances, “SLUDGE”
94
Q

Pyridostigmine

A
  • myasthenia gravis
  • cholinergic enhancers, acetylcholinterase inhibitors (reversible AChE inhibitors), tend not to cross BBB
  • GI disturbances, “SLUDGE”
95
Q

Tetrabenazine

A
  • Huntington’s Disease
  • VMAT inhibitor, inhibition of dopamine uptake into vesicles, results in the degradation of dopamine
  • neuroleptic malignant syndrome, akathisia
96
Q

Deutetrabenazine

A
  • Huntington’s Disease, also receives the indication for Tardive dyskinesia
  • inhibition of dopamine uptake into vesicles, results in the degradation of dopamine, longer half life
  • neuroleptic malignant syndrome, akasthesia
97
Q

Risperidone

A
  • Huntington’s Disease
  • dopamine antagonist, inhibition of D2 receptors
  • drug induced Parkinson’s like Behavior
98
Q

Chlordiazepoxide

A
  • anti-anxiety
  • long acting benzodiazepine
  • Potentiate GABAs ability to open the GABAA chloride channel (increase channel opening frequency)
  • dependence, sedation
99
Q

Lorazepam

A
  • anti-anxiety
  • short acting benzodiazepine
  • Potentiate GABAs ability to open the GABAA chloride channel (increase channel opening frequency)
  • dependence, sedation
100
Q

Alprazolam

A
  • anti-anxiety
  • short acting benzodiazepine
  • Potentiate GABAs ability to open the GABAA chloride channel (increase channel opening frequency)
  • dependence, sedation
101
Q

Triazolam

A
  • anti-anxiety
  • short acting benzodiazepine
  • Potentiate GABAs ability to open the GABAA chloride channel (increase channel opening frequency)
  • dependence, sedation
102
Q

Midazolam

A
  • anti-anxiety
  • short acting benzodiazepine
  • Potentiate GABAs ability to open the GABAA chloride channel (increase channel opening frequency)
  • dependence, sedation
103
Q

Pentobarbital

A
  • anti-anxiety
  • barbiturate
  • Increase duration of GABAA chloride channel openings, at high concentrations can open directly
  • sedation, respiratory depression
104
Q

Phenobarbital

A
  • anti-anxiety
  • barbiturate
  • Increase duration of GABAA chloride channel openings, at high concentrations can open directly
  • sedation, respiratory depression
105
Q

Buspirone

A
  • anti-anxiety
  • serotonin agonist
  • partial agonist at 5-HT1a receptors
  • sedation, metabolised by CYP3A4
106
Q

Clonidine

A
  • PTSD
  • decreases NE actions
  • agonist at NE autoreceptors (alpha2), inhibits the release of more NE
  • hypotension
107
Q

Propranolol

A
  • PTSD
  • drugs that decrease NE actions
  • antagonists at beta adrenergic receptors, blocks NE activity at beta receptors
  • broncos-ask, bradycardia
108
Q

Atomoxetine

A
  • ADHD
  • inhibits the reuptake of NE
  • sexual and GI disturbances
109
Q

Methylphenidate

A
  • ADHD
  • inhibits the reuptake of dopamine and NE
  • difficulty sleeping, mood swings
110
Q

Dextroamphetamine and amphetamine

A
  • ADHD
  • inhibits the reuptake of dopamine and NE as well as may cause the release of some DA and NE
  • difficulty sleeping, mood swings
111
Q

Guanfacine

A
  • ADHD
  • agonist at NE
  • hypotension, drowsiness
112
Q

Imipramine

A
  • antidepressant
  • TCA
  • NE and serotonin reuptake inhibitors
  • sedative, antimuscarinic
113
Q

Amitriptyline

A
  • antidepressant, also approved fo neuropathic pain and fibromyalgia
  • TCA
  • NE and serotonin reuptake inhibitors
  • sedative, antimuscarinic
114
Q

Clomipramine

A
  • antidepressant, also approved for OCD (adults and children >10yr)
  • TCA
  • NE and serotonin reuptake inhibitors
  • sedative, antimuscarinic
115
Q

Desipramine

A
  • antidepressant, also approved for childhood bed wetting and neuropathic pain
  • TCA
  • NE and serotonin reuptake inhibitors, inhibits NE&raquo_space;than serotonin reuptake
  • sedative, antimuscarinic
116
Q

Nortriptyline

A
  • antidepressant
  • second generation TCA
  • NE and serotonin reuptake inhibitor
  • sedative, antimuscarinic
117
Q

Amoxapine

A
  • anti depressant
  • second generation TCA
  • NE and serotonin reuptake inhibitors, antagonist at alpha 1, H1, D2, D4 and 5-HT receptors
  • sedative, antimuscarinic
118
Q

Mirtazapine

A
  • anti depressant
  • further generation of novel cyclic antidepresssant
  • alpha 2 antagonism, 5-HT2 and 5-HT3 antagonism, H1 antagonism
  • sedative, weight gain
119
Q

Bupropion

A

•anti depressant
Further generation of novel cyclic antidepressant
•dopamine reuptake inhibitor, NE&raquo_space;serotonin reuptake inhibitor, antagonist at nicotinic receptors
•dizziness, seizures at high doses

120
Q

Venlafaxine

A
  • anti depressant
  • serotonin and NE reuptake inhibitor, SNRI
  • selectively inhibits NE and 5-HT uptake
  • strong sexual and GI disturbances
121
Q

Duloxetine

A
  • anti depressant, also approved for some types of anxiety and neuropathic pain and fibromyalgia
  • serotonin and NE reuptake inhibitor, SNRI
  • selectively inhibits NE and 5-HT uptake
  • strong sexual and GI disturbances
122
Q

Fluoxetine

A
  • anti depressant, also approved for OCD (adults and children > 7 yr) and PTSD
  • SSRI
  • strong sexual and GI disturbances
123
Q

Paroxetine

A
  • anti depressant, also approved for OCD (adults only) and PTSD
  • SSRI
  • strong sexual and GI disturbances
124
Q

Sertraline

A
  • anti depressant, also approved for PTSD
  • SSRI
  • strong sexual and GI disturbances
125
Q

Fluvoxamine

A
  • anti depressant, also approved for PTSD and OCD (adults and children > 8yr)
  • SSRI
  • strong sexual and GI disturbances
126
Q

Citalopram

A
  • anti depressant
  • SSRI
  • strong sexual and GI disturbances
127
Q

Escitalopram

A
  • anti depressant, also approved for PTSD
  • SSRI
  • strong sexual and GI disturbances
128
Q

Trazadone

A
  • anti depressant
  • second generation serotonin antagonist and reuptake inhibitors, SARI
  • antagonist at 5-HT2 receptors and alpha 1 antagonist, some serotonin reuptake inhibition, partial agonist activity at 5HT1A
  • sedative
129
Q

Vilazodone

A
  • anti - depressant
  • serotonin reuptake inhibitor SARI, partial agonist at 5-HT1A receptors
  • GI disturbances
130
Q

Phenelzine

A
  • anti-depressant
  • MAOi, inhibits the breakdown of NE, serotonin and dopamine
  • serotonin syndrome
131
Q

Selegine

A
  • anti-depressant
  • MAOi, selective for MAO-B, also inhibits dopamine breakdown
  • sedation, hypotension, serotonin syndrome
132
Q

Lithium

A
  • mood stabiliser
  • inhibits neuronal PI turnover inhibiting second messenger activity
  • hypothyroidism, nephrotoxicity
133
Q

Fluphenazine

A
  • antipsychotic
  • typical, antagonist at dopamine D2, D4, D1, adrenergic alpha 1, serotonin 5-HT2, histamine H1, muscarinic receptors
  • extrapyramidal reactions (tardive dyskinesia), neuroleptic malignant syndrome
134
Q

Haloperidol

A
  • antipsychotic
  • typical, antagonist at dopamine D2, D4, D1, adrenergic alpha 1, serotonin 5-HT2, histamine H1, muscarinic receptors
  • extrapyramidal reactions (tardive dyskinesia), neuroleptic malignant syndrome
135
Q

Risperidone

A
  • antipsychotic
  • atypical, antagonist at dopamine D2, D4, adrenergic alpha 1, serotonin 5-HT2, histamine H1,
  • less extrapyramidal reactions, sedation
136
Q

Olanzepine

A
  • antipsychotic
  • atypical, antagonist at serotonin 5-HT2, dopamine D2, D4, muscarinic, histamine H1, adrenergic alpha 1, receptors
  • less extrapyramidal reactions, sedation
137
Q

Aripiprazole

A
  • antipsychotic
  • antagonist at 5-HT2, yet partial agonist at dopamine D2 and serotonin 5-HT1a
  • less extrapyramidal reactions
138
Q

Clozapine

A
  • antipsychotic
  • antagonist at serotonin 5-HT2, dopamine D4, histamine H4,muscarinic, adrenergic alpha 1 receptors
  • less extrapyramidal reactions, sedation
139
Q

Quetiapine

A
  • antipsychotic
  • antagonist at serotonin 5-HT2A, dopamine D2, histamine H1, adrenergic alpha 1 receptors, yet partial agonist at 5-HT1A
  • less extrapyramidal reactions, sedation
140
Q

Donepezil

A
  • Alzheimer’s Disease
  • acetylcholinesterase inhibitors, cross the BBB
  • inhibits the breakdown of acetylcholine, hence more acetylcholine remains in the synapse
  • SLUDGE, difficulty sleeping
141
Q

Rivastigmine

A
  • Alzheimer’s Disease
  • acetylcholinesterase inhibitors, cross the BBB
  • inhibits the breakdown of acetylcholine, hence more acetylcholine remains in the synapse
  • SLUDGE, difficulty sleeping
142
Q

Memantine

A
  • Alzheimer’s Disease
  • glutamate NMDA receptor antagonist
  • blocks the open state of NMDA glutamate channels causing a decrease in the influx of calcium
  • confusion, dizziness
143
Q

Modafinil

A
  • narcolepsy and shift sleep disorder
  • increase the release of NE, DA and histamine by possibly increasing orexin (hypocretin) neuron activity
  • SJS, TENs, induces CYP3A4
144
Q

Zaleplon

A
  • insomnia, non-benzodiazepam sedative/hypnotics
  • potentiate GABAs ability to open the GABA A chloride channel (increase channel opening frequency), very short acting
  • dizziness
145
Q

Zolpidem

A
  • insomnia, non-benzodiazepam sedative/hypnotics
  • potentiate GABAs ability to open the GABA A chloride channel (increase channel opening frequency), short acting
  • dizziness
146
Q

Eszopiclone

A
  • insomnia, non-benzodiazepam sedative/hypnotics
  • potentiate GABAs ability to open the GABA A chloride channel (increase channel opening frequency), long acting
  • dizziness
147
Q

Suvorexant

A
  • insomnia
  • orexin antagonist
  • dizziness
148
Q

Ram elite on

A
  • insomnia
  • melatonin agonist
  • melatonin MT1 and MT2 receptor agonist
  • hyperprolactinemia, possible teratogen
149
Q

Desflurane

A
  • general anaesthetic to maintain anesthesia, most rapid onset and offset
  • halogenated volatile gas
  • Enhance GABA at the GABAA chloride channel & may enhance glycine at glycine channels. Some potassium channel agonist activity.
  • airway irritation, malignant hyperthermia
150
Q

Sevoflurane

A
  • general anaesthetic to maintain anesthesia, rapid onset and offset
  • halogenated volatile gas
  • Enhance GABA at the GABAA chloride channel & may enhance glycine at glycine channels. Some potassium channel agonist activity.
  • airway irritation, malignant hyperthermia
151
Q

Isoflurane

A
  • general anaesthetic to maintain anesthesia, relatively rapid onset and offset
  • halogenated volatile gas
  • Enhance GABA at the GABAA chloride channel & may enhance glycine at glycine channels. Some potassium channel agonist activity.
  • airway irritation, malignant hyperthermia
152
Q

Enflurane

A
  • general anaesthetic to maintain anesthesia, relatively slow onset and offset
  • halogenated volatile gas
  • Enhance GABA at the GABAA chloride channel & may enhance glycine at glycine channels. Some potassium channel agonist activity.
  • airway irritation, malignant hyperthermia
153
Q

Nitrous Oxide

A
  • general anaesthetic to maintain anesthesia, very rapid onset and offset, can be used with halogenated anesthetics to induce anesthesia, weak anaesthetic alone but does have analgesic properties
  • volatile gas
  • inhibit glutamate gated NMDA ion channels, some potassium channel agonist activity
  • increase intracranial pressure
154
Q

Propofol

A
  • general anesthetic
  • IV administered anaesthetic
  • enhance GABA at the GABA A chloride channel and may enhance glycine at clycine channels
  • decrease in cardiac and respiratory function
155
Q

Thiopental

A
  • general anesthetic, barbiturate
  • IV administered
  • increase duration of GABA A chloride channel openings, at high concentrations can open directly
  • respiratory depression
156
Q

Etomidate

A
  • general anesthetic
  • unlike propofol and barbiturates does not decrease cardiac output
  • enhance GABA at the GABA A chloride channel and may enhance glycine at glycine channels
  • decrease in cerebral blood flow and intracranial pressure
157
Q

Ketamine

A
  • general anesthetic
  • causes dissociative anesthesia (analgesia, unresponsive to command and amnesia, yet have their eyes open, move limbs involuntarily and breathe spontaneously)
  • inhibit glutamate gated NMDA ion channels
  • increases in cerebral blood flow and intracranial pressure

Nervous System (11 decks)

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