Pharmacology2

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Pharmacology2
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Drugs covered in Pharmacology
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  1. Diazepam
    • Benzodiazepine
    • Anxiolytic/muscle relaxant/anticonvulsant
    • Bind to the alpha subunit of the GABAA receptor in the CNS
    • - alpha-1: sedation and amnesia
    • - alpha-2: anxiolytic
    • Enhance activation of GABAA mediated chloride channels
    • Long acting
    • Lipid soluble
    • Well absorbed orally
    • Side effects: drowsiness, confusion, amnesia, impaired coordination, potentiate depressant effects of other drugs, tolerance and dependence

    Can be used i.v. as an anticonvulsant
  2. Buspirone
    • Anxiolytic
    • Partial 5-HT1A receptor agonist - reduce 5HT synthesis/release
    • Non-sedative, non-drowsy
    • Takes several weeks to work - alteration in receptor number?
    • Ineffective at treating acute attacks
    • Side effects: nausea, dizziness, headache (doesnt cause sedation or drowsiness
  3. Fluoxetine
    • SSRI
    • Antidepressant/depression associated with anxiety/OCD/panic disorders
    • Leads to receptor downregulation due to increased 5HT in synapse
  4. Paroxetine
    • SSRI
    • Antidepressant/depression associated with anxiety/OCD/panic disorders
    • Leads to receptor downregulation due to increased 5HT in synpase
  5. Citalopram
    • SSRI
    • Antidepressant/depression associated with anxiety/OCD/panic disorders
    • Leads to receptor downregulation due to increased 5HT in synpase
  6. Sertaline
    • SSRI
    • Antidepressant/depression associated with anxiety/OCD/panic disorders
    • Leads to receptor downregulation due to increased 5HT in synpase
  7. Pentobarbital
    • Barbiturate
    • Sleeping tablet
    • Popular in 60's
    • Enhance action of GABA
    • Side effects: repiratory and CV depression on OD, induce CYP450, high degree of tolerance and dependence
  8. Phenobarbital
    • Barbiturate
    • Anticonvulsant
    • Control of seizure by i.v. administration, ineffective in absence seizures
    • Enhance activation of GABAA mediated chloride channels
    • Plasma t1/2 = 50 - 140 h
    • Side effects: repiratory and CV depression on OD, induce CYP450, high degree of tolerance and dependence, sedation, megaloblastic anaemia, osteomalacia
  9. Thiopental
    • Barbiturate CNS depressant
    • I.v. anaesthetic
    • Enhance action of GABA

    • Advantages:
    • Very lipid soluble - rapid induction
    • Rapid redistribution into tissues - blood concentrationd declines rapidly
    • Recovery within 5 minutes

    • Disadvantages:
    • Slowly distributes into fat - long lasting hangover
    • No analgesic effect
    • Profound cardiac and repiratory depression
    • Negative ionotrope - inc HR, coronary blood flow and cardiac demand, pooling of blood in peripheral veins, hypotension in hypovolaemic patients
    • Tissue necrosis or arterial spasm - gangrene

    C/I in: low circulating blood vol, cardiac disease, asthma (bronchospasm)
  10. Alprazolam
    • Benzodiazepine (Xanax)
    • Anxiolytic
    • Antidepressant
    • Bind to the alpha subunit of the GABAA receptor in the CNS
    • - alpha-1: sedation and amnesia
    • - alpha-2: anxiolytic
    • Medium acting
    • Lipid soluble
    • Well absorbed orally
  11. Chlordiazepoxide
    • Benzodiazepine
    • Anxiolytic/muscle relaxant/anticonvulsant
    • Bind to the alpha subunit of the GABAA receptor in the CNS
    • - alpha-1: sedation and amnesia
    • - alpha-2: anxiolytic
    • Side effects: drowsiness, confusion, amnesia, impaired coordination, potentiate depressant effects of other drugs, tolerance and dependence
    • Well absorbed orally
    • Lipid soluble, accumulate in fat
    • Long acting
  12. Lorazepam
    • Benzodiazepine
    • Hypnotic/anxiolytic
    • Bind to the alpha subunit of the GABAA receptor in the CNS
    • - alpha-1: sedation and amnesia
    • - alpha-2: anxiolytic
    • Short acting

    Side effects: drowsiness, confusion, amnesia, impaired coordination, potentiate depressant effects of other drugs, tolerance and dependence
  13. Oxazepam
    • Benzodiazepine
    • Anxiolytic/hypnotic
    • Bind to the alpha subunit of the GABAA receptor in the CNS
    • - alpha-1: sedation and amnesia
    • - alpha-2: anxiolytic
    • Short acting
    • Side effects: drowsiness, confusion, amnesia, impaired coordination, potentiate depressant effects of other drugs, tolerance and dependence
  14. Phenytoin
    • Anticonvulsant
    • Na channel blocker: use dependent block (block inactivated state)
    • Preferentially block cells firing repeatedly (as in seizure) normal activity not compromised
    • Good for partial/generalised siezures, not absence seizures
    • Good oral absorption
    • 80%-90% plasma protein bound (albumin)
    • Side effects: vertigo, ataxia, headache, nystagmus
    • (high dose) confusion, intelluctual effects, gum hyperplasia, hirsutism, acne, megaloblastic anaemia
    • Don't give to adolescents
  15. Carbamazepine
    • Anticonvulsant
    • Na channel blocker: use dependent block (block inactivated state)
    • Preferentially block cells firing repeatedly (as in seizure) normal activity not compromised
    • Effective in most types except absence seizures, also can be used for manic depressive illness
    • Hepatic inducer
    • Side effects: dizziness, drowsiness, ataxia, nausea, vominting,
    • Severe: mental and motor disturbances
  16. Lamotrigne
    • Anticonvulsant
    • Na channel blocker: use dependent block (block inactivated state)
    • Preferentially block cells firing repeatedly (as in seizure) normal activity not compromised
  17. Valproate
    • Anticonvulsant
    • Mildly inhibits GABA activation enzymes (GABA transaminase, SSA dehydrogenase)
    • Some Na channel inhibition: use dependent block (block inactivated state)
    • Enhances post synaptic action of GABA
    • Preferentially block cells firing repeatedly (as in seizure) normal activity not compromised
    • Drug of choice for primary generalised seizures, absence seizures, myoclonic seizures, patients with "grand mal" and "petit mal", infantile epilepsy
    • Side effects: thinning and curling of hair, hepatotoxicity, teratogenic
  18. Ethosuxamide
    • Anticonvulsant
    • Ca channel blocker -T type
    • Treats absence seizures
    • Plasma t1/2 = 50h
    • Side effects: nausea, anorexia, lethargy, dizziness, may precipitate tonic clonic seizures in susceptible patients, rare hypersensitivity reactions
  19. Chlorpromazine
    Dopamine antagonist

    Can be used to treat Huntington's disease (readdress balance)

    Treats schizophrenia - typical antipsychotic

    Side effects: sedation, atropinic side effects, motor side effects
  20. Bicuculline
    • GABA antagonist
    • CNS stimulant/convulsant
    • Lab tool to model epilepsy, no clinical use
  21. Gabapentin
    • Anticonvulsant
    • Mechanism not entirely clear
    • May block calcium channel - L type contriubuting factor, not main drug action
    • May bind to amino acid transporter
    • Treats seizures - adjunctive therapy
    • Plasma t1/2 = 6h
    • Relatively free from side effects
  22. Strychnine
    Antagonist at glycine receptors on motorneurones

    Cause skeletal mucle spasm
  23. Tubocurarine
    Blocks post synaptic ACh receptors
  24. Memantine
    • Treats Alzheimers disease
    • Block NMDA glutamate receptor
  25. Selegiline
    MAO-B inhibitor

    Prevents dopamine metabolism and so increases the half life of dopamine derived from L-dopa in the CNS

    No peripheral inhibition of MAO-A - no cheese reaction
  26. Aspirin
    • Antipyretic analgesic
    • Irreversible COX inhibitor
    • Reduced PG production, "thermostat" back to normal
    • Side effects: GIT upset, bronchoconstriction, bleeding problems, Reyes syndrome
    • High dose side effects: CNS stimulation -> hyperventilation -> decreased PCO2 -> respiratory alkalosis, disturbance of cellular metabolism -> increased lactic/ketoacids -> metabolic acidosis
  27. Paracetamol
    • Antipyretic analgesic
    • Reversible, non-competitive COX-3 (CNS isoenzyme) inhibitor
    • Not anti-inflammatory
    • Reduced PG production, "thermostat" back to normal
    • Analgesic and antipyretic effect equivalent to aspirin
    • Regarded as safer, no gastric damage, haemorrhage, or bronchospasm
  28. Ibuprofen
    • Antipyretic analgesic
    • Reversible, competitive COX inhibitor
    • Reduced PG production, "thermostat" back to normal
  29. Nitrous Oxide
    Inhaled anaesthetic

    • Advantages:
    • Excellent analgesia
    • Non flammable
    • Rapid onset and recovery
    • Little or no toxicity
    • Use as adjunct to other inhalation agents to reduce their dose

    • Disadvantages:
    • No skeletal muscle relaxation
    • Weak anaesthetic - not suitable as sole agent
    • Air pockets in closed spaces expand - "bends"
    • Post-anaesthetic hypoxia - dilutes o2 in lungs for a few minutes - flush out with o2 at end of anaesthesia
    • Methionine synthase inactivation (prolonged/repeat exposure) - inhibits DNA and protein synthesis, megaloblastic anaemia and leucopoenia
    • Foetal abnormalities/spontaneous abortion - theatre staff
  30. Halothane
    Inhaled anaesthetic

    Widely used in paediatrics

    • Advantages:
    • Non flammable
    • Potent and high oil:gas partition coefficient
    • Rapid induction
    • Rapid recovery
    • Controlled hypotension to limit bleeding
    • Non-irritant
    • Few post-op effects

    • Disadvantages:
    • Doesn't provide adequate analgesia
    • May not provide adequate muscle relaxation
    • Vasodilator and cardiac depressant -> myocardial depression
    • Highly potent so easy to over anaesthetise
    • Sensitises heart to adrenaline - cardiac dysrhythmias (avoid beta blockers and adrenaline)
    • Respiratory depression
    • Hepatotoxic if repeated exposure (3 months between exposures)
    • Malignant hyperthermia
  31. Desflurane
    Inhaled anaesthetic

    • Advantages:
    • Low solubility in blood
    • Minimal systemic effects
    • Minimal metabolism
    • Few side effects

    • Disadvantages:
    • Expensive
    • Some respiratory tract irritation
  32. Propofol
    I.v. anaesthetic

    • Advantages:
    • Rapid metabolism, rapid recovery, no hangover
    • Can be continuously infused to maintain anaesthesia
    • None of the effects of epotomidate

    • Disadvantages:
    • Rapid metabolism, short duration of action
    • Not water soluble, painful injection
  33. Atropine
    Muscarinic antagonist (competative)
  34. Hyosine
    • Muscarinic antagonist
    • Used for treatment/prevention of motion sickness
    • Less effective after onset
    • Ineffective against substances acting directly on CTZ
    • Side effects: dizziness, dry mouth, blurred vision
  35. Papaveretum
    • Opioid analgesic
    • Mixture
  36. Propranolol
    • Beta blocker
    • Can be used to treat hyperthyroidism
    • Decreases symptoms, but patient still hyperthyroid biochemically
    • Used prior to surgery, in treatment with thyrotoxic crisis, initially with carbimazole, following radiation
  37. Flumazenil
    • Benzodiazepine antagonist
    • Competitive inhibition at the benzodiazepine binding site on the GABAA receptor
  38. Flupentixol
    • Typical antipsychotic
    • Thioxanthine
    • Antagonist at various dopamine (D1-D5), serotonin (5-HT2), adrenaline (α1), and histamine (H1) receptors, without affecting the muscarinic acetylcholine receptors
    • Side effects: slight sedation, slight atropinic side effects, pronounced motor effects
  39. Fluphenazine
    • Typical antipsychotic
    • Piperazine
  40. Theobromine
    Methylxanthine

    Effects: stimulate cardiac and skeletal muscle, relax smooth muscle, induce diuresis, offset fatigue, reduce reaction time

    Least potent

    • Antagonism at adenosine (A2) receptors
    • Inhibition of phosphodiesterase
    • Mobilization of intracellular calcium
  41. Theophylline
    Methylxanthine

    Effects: stimulate cardiac and skeletal muscle, relax smooth muscle, induce diuresis, offset fatigue, reduce reaction time

    Middle potent

    • Antagonism at adenosine (A2) receptors
    • Inhibition of phosphodiesterase
    • Mobilization of intracellular calcium
  42. Thymidine
    DNA nucleoside
  43. Tryptophan
    • Can be used in depression
    • Pre-cursor for 5HT
    • Potentiates effect of MAOI's
    • Limited use: adjunct in mild/moderate depression
  44. Tyramine
    • Monoamine
    • Responsible for Cheese reaction with MAOI's
  45. Tyrosine
    Amino acid
  46. Lithium carbonate
    • Antidepressant
    • Controls both depression and mania, so drug of choice for bi-polar
    • Displaces Na ions
    • Affects inositol phosphate inhibits conversion from IP1 to inositol
    • Has other effects
    • Side effects: tremor, mental confusion, sinus node toxicity, polydipsia, polyuria
    • Narrow TI - levels need monitoring
  47. Acarbose
    • Treats type II diabetes
    • Inhibits alpha glucosidase enzymes which turn complex carbohydrates into glucose
    • Reduces glucose available for absorption
    • No hypoglycaemia
    • No weight gain
  48. Pioglitazone
    • Treats type II diabetes
    • Activates nuclear receptor - PPARy
    • Receptor binds to DNA - increases gene transcription
    • Increase plasmalemmal glucose transporters - increase muscle glucose uptake
    • Reduce liver glucose output
    • Increases lipogenesis, uptake of fatty acids
    • Overall effect increases sensitivity to insulin
    • Slow onset - 1-2 months
    • No increased risk of hypoglycaemia
    • Almost unique metabolic pathway - CYP2C8
    • Rare reports of liver toxicity - monitor
  49. Rosiglitazone
    • Treats type II diabetes
    • Activates nuclear receptor - PPARy
    • Receptor binds to DNA - increases gene transcription
    • Increase plasmalemmal glucose transporters - increase muscle glucose uptake
    • Reduce liver glucose output
    • Increases lipogenesis, uptake of fatty acids
    • Overall effect increases sensitivity to insulin
    • Slow onset - 1-2 months
    • No increased risk of hypoglycaemia
    • Almost unique metabolic pathway - CYP2C8
    • Rare reports of liver toxicity - monitor
  50. Metformin
    • Treats type II diabetes
    • Mechanism unclear
    • - receptor sensitivity?
    • - peripheral glucose uptake?
    • - liver glucose production
    • Requires insulin presence
    • Does not promote insulin release - no risk of hypoglycaemia
  51. Sitagliptin
    • Treats type II diabetes as adjunct
    • Inhibits dipeptidyl peptidase-4
    • - increased levels of incretin
    • - increase insulin release
    • - inhibit glucagon release
    • -slow gastric emptying
  52. Glibenclamide
    • Sulphonylurea
    • Used to treat type II diabetes
    • Stimulates insulin secretion by blocking K+ATP channels in B cells
    • Require functioning B cells
    • Also block other K+ATP channels e.g. vascular smooth muscle
    • T1/2 = 12
    • Side effects: hypoglycaemia, stimulate appetite, drug interactions (NSAIDs, warfarin, antifungals)
  53. Disulfiram
    • Antabuse
    • Blocks the enzyme acetaldehyde dehydrogenase
  54. Levodopa
    Treatment of Parkinson's Disease

    Used because dopamine cannot cross BBB

    Metabolised to dopamine in CNS

    Also in periphery - side effects and reduction in LDOPA in brain
  55. Domperidone
    • D2 receptor antagonist
    • Does cross BBB
    • Reduced side effects
    • Side effects: migraine
  56. Nabilone
    • Cannabinoid antiemetic
    • Treats vomiting caused by cytotoxic anticancer drugs (also as adjuvant for neuropathic pain)
    • Effective against substances which stimulate the CTZ
    • Thought to act via opioid receptors in the CTZ
    • Sometimes effective where other treatment has failed
    • Side effects: drowsiness, dizziness, dry mouth, modd changes, postural hypotension, hallucinations, psychotic reactions
  57. Ondansetron
    • 5HT3 receptor antagonist
    • Used for nausea and vomiting caused by cytotoxic anticancer drugs, post-op vominting and radiation induced vomiting
    • Primary site of action is on the CTZ
    • Side effects: headache, GI upset
  58. Promethazine
    H1 receptor antagonist
  59. Clomiphene
    • Oral non-steroidal
    • Treats women having difficulty conceiving
    • Binds oestrogen receptors
    • - hypothalamus unable to recognise endogenous oestrogen
    • - alters pulsility of GnRH
    • - pituitary gonadotrophin secretion increased
    • - may also affect gonadotrophin secretion directly
    • Side effects: increased risk of multiple pregnancy, visual disturbances, hot flushes, breast tenderness, headache, ovarian cancer?
  60. Levonorgestrel
    • Morning after pill
    • Mechanism unclear
    • - delays ovulation?
    • - prevents implantation?
    • - inhibition of sperm transport?
  61. Mestranol
    • Estrogen combined oral contraceptive
    • Need high dose if used alone
  62. Mifepristone
    • Termination of pregnancy
    • Progesterone antagonist
    • - progesterone receptor/antagonist complex binds DNA and recruit corepressors
    • Used for medical terminations in 1st trimester
  63. Tamoxifen
    • SERM
    • Binds Estrogen receptor - partial agonist
    • Treats breast cancer
  64. Iodine
    • Treats hyperthyroidism
    • Rapid effect, not sustained
    • Inhibits peroxide generation?
    • Inhibits iodination?
    • Decreases size and vascularity of gland
    • Used prior to surgery, treatment of thyrotoxic crisis
    • Allergic responses possible
  65. Propylthiouracil
    • Thioureylene
    • Competitive inhibition of thyroperoxidase enzymes
    • - reduce iodination of tyrosine
    • - reduce T3 and T4 output
    • Treats hyperthyroidism
    • Slow reponse - relapse common
    • Side effects; hypothyroidism, skin rash (less common than carbimazole), granulocytopenia
  66. Galantamine
    Reversible inhibitor of acetylcholinesterase

    Used to treat dementia
  67. Glycine
    Inhibitory CNS transmitter

    Found mostly in spinal cord

    Derived from serine by action of SMHT

    Inactivated by uptake and metabolism

    ACh released by a collateral of the alpha motor neurone which acts on nicotinic receptors of the Renshaw cell to cause glycine release

    Modulates contraction of skeletal muscle by providing a negative feedback loop by acting on receptor at alpha motor neurone causing hyperpolarisation
  68. GABA
    Main inhibitory transmitter in the brain

    Widespread distribution

    Synthesised from glutamate by GAD

    Inactivated by active uptake

    GABA transaminase converts GABA to succinic semialdehyde (glutamate formed in process)

    Facilitates entry of chloride ions into neurones, resulting in hyperpolarisation (neurone depression)
  69. Glutamate
    Main excitatory transmitter in CNS

    Widely and uniformly located in CNS

    Formed from alpha-oxoglutarate (Krebs cycle) by GABA-aminotransferase

    Inactivated by active uptake

    Actions exerted via receptors
  70. Haloperidol
    Dopamine antagonist

    Can be used to treat Huntington's disease (readdress balance between dopamine and GABA)

    Treats schizoprenia - typical antipsychotic
  71. Raloxifene
    • SERM
    • Binds Estrogen receptor
    • Treats breast cancer
  72. Tetanus toxin
    Inhibits glycine release

    Causes uncontrollable muscle spasm
  73. GABA A receptors
    Ligand gated ion channel

    Pentamer structure with alpha, beta and gamma subunits

    Located post-synaptically

    Activation opens Cl- channels which reduced membrane excitability

    Several binding sites (barbiturates, benzodiazepines, GABA)
  74. GABA B receptors
    G protein coupled receptor

    Linked to adenylyl cyclase

    Inhibit cAMP formation

    Located pre and post synaptically (results in pre and post synaptic inhibition)

    Prevents Ca2+ channel opening

    Increases K+ permeability
  75. Ionotropic Glutamate receptors
    ligand gated cation channels

    Named after specific agonists (NMDA, AMPA and kainate)

    Pentameric structure

    NMDA and AMPA are post-synaptic

    Kainate is pre and post synaptic

    NMDA and possibly AMPA have modulatory sites (glycine binds to NMDA)

    Cause slow (NMDA) or fast (AMPA) EPSP
  76. NMDA receptor
    Highly permeable to Ca2+

    Blocked by Mg2+

    Blocked by some anaesthetics (ketamine)

    Blocked by some psychomimetics (phencyclidine)
  77. Metabotropic receptors
    G protein coupled receptor

    No homology with other GPCR

    linked to intracellular second messenger systems (phospholipase C) which result in IP3 production and release of Ca2+
  78. Acetylcholine
    Widely distributed in CNS - cortex, basal ganglia, brainstem, spinal cord

    Main excitatory action

    Inactivated by acetylcholinesterases
  79. Nicotinic receptors
    Ligand gated ion channels

    Pentameric

    alpha and beta subunits

    pre-synaptic

    facilitate release of other transmitters (glutamate and dopamine)

    activated by acetylcholine
  80. Muscarinic receptors
    GPCR

    M1 class

    activate phospholipase C
  81. Donepezil
    Reversible inhibitor of acetylcholinesterase

    Used in treatment of dementia
  82. Rivastigmine
    Reversible inhibitor of acetylcholinesterase

    Used in treatment of dementia
  83. Noradrenaline in CNS
    Synthesis, storage, release, inactivation as in PNS

    Mainly inhibitory via beta, but some excitatory via alpha and beta

    Involved in blood pressure regulation

    Important in mood, arousal and reward pathways
  84. Serotonin in the CNS
    Derived from tryptophan (diet)

    Similar pathway to NA - tryptophan dehydroxylase, NH2 acid decarboxylase

    Inactivated by uptake and metabolism by MAO, aldehyde dehydrogenase

    Roles in: hallucinations, behaviour, sleep, wakefulness, body temperature, sensory pathways, vomiting (5HT3), mood, emotion
  85. Serotonin receptors
    7 subtypes

    All GPCR except 5HT3 which is a ligand gated ion channel

    • 5HT1,2,3 appear to be the most important in CNS
    • 1. linked to cAMP (inhibitorys)
    • 2. linked to IP3/DAG (excitatory)
    • 3. excitatory
  86. Dopamine
    Synthesis via dopamine beta-hydroxylase

    Tyrosine to dopa is controlled by tyrosine hydroxylase (rate limiting step)

    Inactivated by selective active re-uptake, metabolism by MAO-B and COMT to DOPAC and HVA

    Found in nigrostrital pathway (motor control), mesolimbic/mesocortical (behavioural effects) pathway, tubero-hypophyseal (endocrine) pathway
  87. Dopamine receptors
    Two types:

    • D1 type (D1 and D5)
    • GPCR linked to adenylyl cyclase
    • increase cAMP
    • Mainly post-synaptic inhibition

    • D2 type (D2, D3, D4)
    • GPCR linked to adenylyl cyclase
    • Decrease cAMP
    • pre and post synaptic inhibition
    • Mediate most known CNS functions of DA
  88. Entacapone
    COMT inhibitor

    Co administered with L-DOPA to reduce peripheral DOPA metabolism to treat Parkinsons
  89. Carbidopa
    Peripheral dopa decarboxylase inhibitor

    Prevents conversion of L-dopa to dopamine in peripheral tissues

    Do not cross BBB

    Reduces peripheral side effects and increases L-dopa dose getting into the brain
  90. Benserazide
    Peripheral dopa decarboxylase inhibitor

    Prevents conversion of L-dopa to dopamine in peripheral tissues

    Do not cross BBB

    Reduces peripheral side effects and increases L-dopa dose getting into the brain
  91. Pergolide
    Ergot derivative dopamine agonist

    Act directly at D2 receptors

    Can be used in the treatment of Parkinson's

    Cause nausea (action at CTZ) - reduce by administration of domperidone
  92. Bromocriptine
    Ergot derivative dopamine agonist

    Act directly at D2 receptors

    Can be used in the treatment of Parkinson's

    Cause nausea (action at CTZ) - reduce by administration of domperidone
  93. Cabergolide
    Ergot derivative dopamine agonist

    Act directly at D2 receptors

    Can be used in the treatment of Parkinson's

    Cause nausea (action at CTZ) - reduce by administration of domperidone
  94. Lisuride
    Ergot derivative dopamine agonist

    Act directly at D2 receptors

    Can be used in the treatment of Parkinson's

    Cause nausea (action at CTZ) - reduce by administration of domperidone
  95. Pramipexol
    Dopamine agonist

    Non-ergot derivative

    Act directly at D2 receptors

    Treats Parkinson's

    Cause nausea (action at CTZ) - reduce by administration of domperidone
  96. Ropinirole
    Dopamine agonist

    Non-ergot derivative

    Act directly at D2 receptors

    Treats Parkinson's

    Cause nausea (action at CTZ) - reduce by administration of domperidone
  97. Apomorphine
    Dopamine agonist

    Non-ergot derivative

    Act directly at D2 receptors

    Cause nausea (action at CTZ) - reduce by administration of domperidone

    Treats Parkinson's
  98. Amantadine
    Anti-viral drug

    However also has weak anti-Parkinson's action

    • Mechanism unclear;
    • Increase dopamine release?
    • Inhibit dopamine uptake?
    • Agonis activity at D2 receptors?
  99. Benzatropine
    Muscarinic antagonist

    Treats Parkinson's

    More effective against tremor than hypokinesia

    Antimuscarinic side effects due to peripherally blocked muscarinic receptors

    Worsen signs of dementia - C/I
  100. Orphenadrine
    Muscarinic antagonist

    Treats Parkinson's

    More effective against tremor than hypokinesia

    Antimuscarinic side effects due to peripherally blocked muscarinic receptors

    Worsen signs of dementia - C/I
  101. Tetrabenazine
    Treats Huntington's

    Mechanism unclear - depletes dopamine to readdress balance?
  102. Baclofen
    GABA B agonist

    Treats Huntington's
  103. Enflurane
    Inhaled anaesthetic

    • Advantages:
    • Stable
    • Non flammable
    • Potency/induction similar to halothane

    • Disadvantages:
    • Dose related depression of myocardial contractility
    • Produces fluoride ions - renal toxicity
    • Lowers threshold for seizures
    • Known to cause malignant hypothermia
  104. Isoflurane
    Inhaled anaesthetic

    Widely used

    • Advantages:
    • No metabolism - little toxicity
    • Not pro-convulsive
    • Excellent muscle relaxant

    • Disadvantages:
    • Expensive
    • Hypotension
    • Coronary vasodilator
  105. Sevoflurane
    Inhaled anaesthetic

    • Advantages:
    • More potent then desflurane
    • Less respiratory irritation

    • Disadvantages:
    • Expensive
    • Partially metabolised
  106. Etomidate
    • I.v. anaesthetic
    • GABA receptor agonist - CNS depressant
    • Induction agent only

    • Disadvantages:
    • No analgesic activity
    • Mild dose related respiratory depression
    • Decreased cerebral metabolism
    • Pain on injection (propylene glycol)
    • Myoclonic activity
    • Cortisol suppression
    • Post-op nausea and vomiting

    Favoured over thiopental - large margin between anaesthetic dose and resp/CV depression also faster metabolism, less hungover
  107. Triazolam
    • Benzodiazepine
    • Anxiolytic
    • Bind to the alpha subunit of the GABAA receptor in the CNS
    • - alpha-1: sedation and amnesia
    • - alpha-2: anxiolytic
    • Ultra short acting
    • Lipid soluble
    • Well absorbed orally
    • Side effects: drowsiness, confusion, amnesia, impaired coordination,
    • potentiate depressant effects of other drugs, tolerance and dependence
  108. Midazolam
    • Benzodiazepine
    • Anxiolytic
    • Bind to the alpha subunit of the GABAA receptor in the CNS
    • - alpha-1: sedation and amnesia
    • - alpha-2: anxiolytic
    • Ultra short acting
    • Lipid soluble
    • Well absorbed orally
    • Side effects: drowsiness, confusion, amnesia, impaired coordination,
    • potentiate depressant effects of other drugs, tolerance and dependence

    Can be used i.v. in anaesthesia
  109. Zolpidem
    • Benzodiazepine
    • Hypnotic
    • Bind to the alpha subunit of the GABAA receptor in the CNS
    • - alpha-1: sedation and amnesia
    • - alpha-2: anxiolytic
    • Ultra short acting
    • Lipid soluble
    • Well absorbed orally
    • Side effects: drowsiness, confusion, amnesia, impaired coordination,potentiate depressant effects of other drugs, tolerance and dependence
  110. Temazepam
    • Benzodiazepine
    • Anxiolytic/hypnotic
    • Bind to the alpha subunit of the GABAA receptor in the CNS
    • - alpha-1: sedation and amnesia
    • - alpha-2: anxiolytic
    • Short acting
    • Lipid soluble
    • Well absorbed orally
    • Side effects: drowsiness, confusion, amnesia, impaired coordination,potentiate depressant effects of other drugs, tolerance and dependence
  111. Lometazepam
    • Benzodiazepine
    • Anxiolytic/hypnotic
    • Bind to the alpha subunit of the GABAA receptor in the CNS
    • - alpha-1: sedation and amnesia
    • - alpha-2: anxiolytic
    • Short acting
    • Lipid soluble
    • Well absorbed orally
    • Side effects: drowsiness, confusion, amnesia, impaired coordination,potentiate depressant effects of other drugs, tolerance and dependence
  112. Nitrazepam
    • Benzodiazepine
    • Anxiolytic/hypnotic
    • Bind to the alpha subunit of the GABAA receptor in the CNS
    • - alpha-1: sedation and amnesia
    • - alpha-2: anxiolytic
    • Medium acting
    • Lipid soluble
    • Well absorbed orally
    • Side effects: drowsiness, confusion, amnesia, impaired coordination,potentiate depressant effects of other drugs, tolerance and dependence
  113. Flurazepam
    • Benzodiazepine
    • Anxiolytic
    • Bind to the alpha subunit of the GABAA receptor in the CNS
    • - alpha-1: sedation and amnesia
    • - alpha-2: anxiolytic
    • Long acting
    • Lipid soluble
    • Well absorbed orally
    • Side effects: drowsiness, confusion, amnesia, impaired coordination,potentiate depressant effects of other drugs, tolerance and dependence
  114. Clonazepam
    • Benzodiazepine
    • Anxiolytic/anticonvulsant
    • Bind to the alpha subunit of the GABAA receptor in the CNS
    • - alpha-1: sedation and amnesia
    • - alpha-2: anxiolytic
    • Long acting
    • Lipid soluble
    • Well absorbed orally
    • Side effects: drowsiness, confusion, amnesia, impaired coordination,potentiate depressant effects of other drugs, tolerance and dependence
  115. Tiagabine
    • Anticonvulsant
    • Enhances GABA action by inhibiting uptake - GABA analogue
    • Adjunctive therapy for partial seizures
    • Effective in patients resistant to established drugs
    • Side effects: drowsiness, confusion
  116. Vigabatrin
    • Anticonvulsant
    • Enhances GABA action by irreversibly inhibiting GABA transaminase (breakdown to succinic semialdehyde)
    • Increases GABA and inhibitory transmission
    • Treats simple complex generalised, tonic clonic seizures
    • 1st "designer" epilepsy drug
    • Short plasma t1/2 but long lasting effect
    • Side effects: rare - depression and psychotic disturbances
  117. Pregabalin
    • Pro-drug
    • Similar to gabapentin but less side effects
    • Mechanism not clear
    • May block Ca channel
    • May bind to amino acid transporter
  118. Ozcarbamazepine
    • Pro-drug
    • Anticonvulsant
    • Metabolised to a compound sinilar to carbamazepine
    • Na channel blocker
  119. Amphetamine
    • Stimulant
    • Displaces vesicular monoamine while inhibiting MAO and monoamine reuptake
    • Indirect receptor activation
    • Effects: vasoconstriction, mydriasis, inhibition of GIT and urinary bladder, alertness, increased motor activity, anorexia, anxiety (due to overstimulation of brain)
  120. Fenfluramine
    • Weight loss drug
    • Amphetamine
    • Did not produce CNS side effects
    • Withdrawn due to cardiac effects
  121. Dexamphetamine
    • Amphetamine
    • Treats hyperkinesia and narcolepsy
  122. Methylphenidate
    • Ritalin
    • Amphetamine
    • Treats hyperkinesis and narcolepsy
  123. Picrotoxin
    • GABA antagonist
    • CNS stimulant/convulsant
    • Lab to model epilepsy
    • No clinical use
  124. Doxapram
    • Analeptic
    • Previously used to treat drug induced repiratory depression
    • CNS mechanism unknown
    • Peripheral mechanism, only one still used
  125. Bemeglide
    • Analeptic
    • Previously used to treat drug induced repiratory depression
    • CNS mechanism unknown
    • No longer used
  126. Nikethamide
    • Analeptic
    • Previously used to treat drug induced repiratory depression
    • CNS mechanism unknown
    • No longer used
  127. Caffeine
    Methylxanthine

    Effects: stimulate cardiac and skeletal muscle, relax smooth muscle, induce diuresis, offset fatigue, reduce reaction time

    Most potent

    • Antagonism at adenosine (A2) receptors
    • Inhibition of phosphodiesterase
    • Mobilization of intracellular calcium
  128. Haloperidol
    • Typical antipsychotic
    • Butyrophenone
    • Antagonism at dopamine receptors, 5HT and histamine receptors
    • Pronounced motor effects
  129. Pimozide
    • Atypical antipsychotic
    • Diphenylbutylpiperidine
  130. Thioridazine
    • Atypical antipsychotic
    • Phenothiazines piperidines
  131. Clozapine
    Atypical antipsychotic

    • Lower chance of extrapyridamol side effects
    • Mechanism uncertain
    • D1 D2 5HT2 H1 ACh alpha-2 receptors blocked

    Potentially fatal haematological side effects
  132. Risperidone
    Atypical antipsychotic

    • Lower chance of extrapyridamol side effects
    • Mechanism uncertain
    • D1 D2 5HT2 H1 ACh alpha-2 receptors blocked
  133. Olanzapine
    Atypical antipsychotic

    • Lower chance of extrapyridamol side effects
    • Mechanism uncertain
    • D1 D2 5HT2 H1 ACh alpha-2 receptors blocked
  134. Sertindole
    Atypical antipsychotic

    • Lower chance of extrapyridamol side effects
    • Mechanism uncertain
    • D1 D2 5HT2 H1 ACh alpha-2 receptors blocked
  135. Zotepine
    Atypical antipsychotic

    • Lower chance of extrapyridamol side effects
    • Mechanism uncertain
    • D1 D2 5HT2 H1 ACh alpha-2 receptors blocked
  136. Phenelzine
    • MAOI
    • Irreversible inhibitor
    • Indicated in psychotic and neurotic depression
    • Take over 3 weeks to work
    • Limited use

    Side effects: convulsions, excitement (related to amphetamine), hepatoxiicity, pyrexia, hypertensive crisis i.e. cheese reaction
  137. Tranylcypromine
    • MAOI
    • Slowly reversible inhibitor
    • Indicated in psychotic and neurotic depression
    • Take over 3 weeks to work
    • Limited use

    Side effects: convulsions, excitement (related to amphetamine), hepatoxiicity, pyrexia, hypertensive crisis i.e. cheese reaction
  138. Moclobemide
    • MAOI
    • Reversible inhibitor
    • Indicated in psychotic and neurotic depression
    • Take over 3 weeks to work
    • Limited use

    Side effects: convulsions, excitement (related to amphetamine), hepatoxiicity, pyrexia, hypertensive crisis i.e. cheese reaction
  139. Amitrypyline
    • Monoamine uptake inhibitor
    • Tricyclic antidepressant
    • Antidepressant drug of choice
    • 2-4 weeks to work
    • Inhibits NA and 5HT uptake
    • Antagonist at muscarininc receptors - dry mouth, blurred vision, urinary retention, arrhythmias, tachycardia, syncope
  140. Iprindole
    • Monoamine receptor agonist
    • A 5HT agonist?
    • Relieve both psychotic and neurotic depression
  141. Pethidine
    • Opioid analgesic
    • Agonist at opioid receptors
    • More convulsions (metabolite norpethidine)
    • Not dependent on glucuronide conjugation metabolism
  142. Morphine
    • Opioid analgesic
    • Long duration of effect
  143. Fentanyl
    • Opioid analgesic
    • Opioid receptor agonist
    • Short duration of action
    • Side effects: cough suppression
  144. Codeine
    • Opioid analgesic
    • Opioid receptor agonist
    • Weaker activity than morphine
    • More nausea
  145. Heroin
    • Opioid analgesic
    • Opioid receptor agonist
    • More analgesic activity than morphine and faster onset of action
    • Short duration
  146. Naloxone
    • Competitive antagonist at all 3 opioid receptors
    • Used to treat drug induced respiratory depression
    • Short action
    • Precipitate withdrawal
  147. Buprenorphone
    • Opioid analgesic
    • Reduced abuse potential
    • Partial agonist at Mu
    • Kappa antagonism
    • Withdrawal less intense than morphine
    • Respiratory depression not fully reversed by naloxone
    • Analgesic and in management of dependence
    • Side effects: sedative, marked nausea and vomiting
  148. Pentazocine
    • Opioid analgestic with reduced abuse potential
    • Limited respiratory depression
    • Mu antagonist
    • Kappa agonist
    • Sigma agonist
    • Prolonged use gives dependence
  149. Pholcodine
    • Cough suppressant
    • Structurally related to opioids - large substituent added at 3 position
    • Little analgesic effect
    • Action at CNS cough centre, via mu and delta receptors?
  150. Dextromethorphan
    • Cough suppressant
    • Structurally related to opioids - large substituent added at 3 position
    • No analgesic effect
    • Not blocked by opioid antagonists
    • Action at CNS cough centre, via mu and delta receptors?
    • Has non opioid binding sites
  151. Meptazinol
    • Opioid analgesic
    • Mu1 selective agonist
    • Less respiratory depression than other opioids
  152. Apomorphine
    • Dopamine agonist
    • Structurally similar to morphine, causes emesis without other opioid actions
    • Used in Parkinson's
  153. Nalorphine
    • Opioid analgesic with lower abuse potential
    • Not used clinically - dysphoria
    • Mu antagonist
    • Delta kappa partial agonist
    • Sigma agonist
  154. Cyclizine
    • Histamine H1 receptor antagonist
    • Used in prevention/treatment of motion sickness
    • Ineffective against substances acting directly on CTZ
    • Side efffects: drowsiness and sedation
  155. Cinnarizine
    • Histamine H1 receptor antagonist
    • Used in prevention/treatment of motion sicknes and treatment of vestibular disorders (Menier's)
    • Ineffective against substances acting directly on CTZ
    • Side effects: drowsiness and sedation
  156. Chloropromazine
    • D2 receptor antagonist
    • Treats nausea and vomiting associated with cancer treatment, radiation therapy, cytotoxics, opioids, post-op nausea, severe morning sickness
    • Pass BBB
    • Also block histamine and mACh receptors
    • Effective after vomiting onset
    • Side effects: sedation, hypotension, dystonia, dyskinesia
  157. Perphenazine
    • D2 receptor antagonist
    • Treats nausea and vomiting associated with cancer treatment, radiation
    • therapy, cytotoxics, opioids, post-op nausea, severe morning sickness
    • Pass BBB
    • Also block histamine and mACh receptors
    • Effective after vomiting onset
    • Side effects: sedation, hypotension, dystonia, dyskinesia
  158. Trifluoroperazine
    • D2 receptor antagonist
    • Treats nausea and vomiting associated with cancer treatment, radiation
    • therapy, cytotoxics, opioids, post-op nausea, severe morning sickness
    • Typical antipsychotic
    • Phenothiazine piperidine
    • Pass BBB
    • Also block histamine and mACh receptors
    • Effective after vomiting onset
    • Side effects: sedation, hypotension, dystonia, dyskinesia
  159. Metoclopramide
    • D2 receptor antagonist
    • Passes BBB
    • Acts on DA receptors throughout CNS
    • Also peripheral prokinetics
    • 2nd line treatment for severe morning sickness
    • Side effects: movement disorder, fatigue, motor restlessness, spasmodic torticolis, occulogyric crisis, menstruation disorder, diarrhoea
  160. Dexamethasone
    • Steroid
    • Glucocorticoid
    • Long acting
    • Treats vomiting caused by cytotoxics
    • Unknown mechanism
    • Used in combo with D2 or 5HT3 receptor antagonists
  161. Neuronkinin-1-antagonist
    • Substance P antagonist
    • Treats vomiting caused by cytotoxics/post-op NV
    • Side effects: hiccuping, fatigue, listlessness, constipation/diarrhoea, loss of appetite, dizziness, ringing in ears
  162. Hydrocortisone
    • Natural steroid
    • Synthesised from cholesterol
    • Control of synthesis and release via hypothalamus, anterior pituitary and negative feedback
    • Shows both glucocorticoid and mineralocorticoid action
    • Enzyme in kidneys etc converts these to mineralo-inactive compounds
    • Short acting
    • Used for replacement therapy in adrenal failure - few side effects as natural situation mimicked, and for anti-inflammatory/immunosuppressant actions
    • Side effects: drug induced Cushing's syndrome (buffalo hump, moon face, inc abdo fat, poor wound healing, osteoporosis, muscle wasting, hypertension, thinning of skin), increased risk of infection, suppression of normal steroid synthesis (abrupt withdrawal can lead to acute adrenal failure)
  163. Prednisolone
    • Synthetic steroid
    • Mixed gluco-/mineralocorticoid action
    • Medium acting
    • Used for asthma
    • Side effects: drug induced Cushing's syndrome (buffalo hump, moon face,
    • inc abdo fat, poor wound healing, osteoporosis, muscle wasting,
    • hypertension, thinning of skin), increased risk of infection,
    • suppression of normal steroid synthesis (abrupt withdrawal can lead to
    • acute adrenal failure)
  164. Betamethasone
    • Synthetic steroid
    • Glucocorticoid
    • Long acting
    • Side effects: drug induced Cushing's syndrome (buffalo hump, moon face,
    • inc abdo fat, poor wound healing, osteoporosis, muscle wasting,
    • hypertension, thinning of skin), increased risk of infection,
    • suppression of normal steroid synthesis (abrupt withdrawal can lead to
    • acute adrenal failure)
  165. Beclomethasone
    • Synthetic steroid
    • Glucocorticoid
    • Long acting
    • Used for asthma
    • Side effects: drug induced Cushing's syndrome (buffalo hump, moon face,
    • inc abdo fat, poor wound healing, osteoporosis, muscle wasting,
    • hypertension, thinning of skin), increased risk of infection,
    • suppression of normal steroid synthesis (abrupt withdrawal can lead to
    • acute adrenal failure)
  166. Budesonide
    • Synthetic steroid
    • Glucocorticoid
    • Used for asthma
    • Side effects: drug induced Cushing's syndrome (buffalo hump, moon face,
    • inc abdo fat, poor wound healing, osteoporosis, muscle wasting,
    • hypertension, thinning of skin), increased risk of infection,
    • suppression of normal steroid synthesis (abrupt withdrawal can lead to
    • acute adrenal failure)
  167. Fludrocortisone
    • Steroid
    • Mainly mineralocorticoid
    • Short acting
    • Side effects: drug induced Cushing's syndrome (buffalo hump, moon face,
    • inc abdo fat, poor wound healing, osteoporosis, muscle wasting,
    • hypertension, thinning of skin), increased risk of infection,
    • suppression of normal steroid synthesis (abrupt withdrawal can lead to
    • acute adrenal failure)
  168. Aminoglutethimide
    • Cancer drug
    • Inhibits conversion of cholesterol to pregnenolone
    • Reduces adrenal output of androgens/oestrogens
    • Used for post-menopausal breast cancer and prostate cancer
    • Require corticosteroid replacement as they are also inhibited
    • Rarely used now
  169. Trilostane
    • Inhibits conversion of pregnenalone to progesterone
    • Reduces output of adrenal steroids
    • Treats Cushings syndrome, hyperaldosterism, postmenopausal breast cancer
  170. Metyrapone
    • Inhibits beta hydroxylation at C11
    • Reduces output of hydrocortisone and CS
    • Treats Cushings syndrome
    • Also reduces -ve feedback so increases ACTH - used to test anterior pituitary function
  171. Tetracosatrin/tetracosatride
    • First 24 aa's of ACTH
    • Stimulates synthesis and release of adrenal hormones
    • Used to diagnose adrenal insufficiency
  172. Gliclazide
    • Sulphonylurea
    • Used to treat type II diabetes
    • Stimulates insulin secretion by blocking K+ATP channels in B cells
    • Require functioning B cells
    • Also block other K+ATP channels e.g. vascular smooth muscle
    • T1/2 = 7h
    • Side effects: hypoglycaemia, stimulate appetite, drug interactions (NSAIDs, warfarin, antifungals)
  173. Tolbutamide
    • Sulphonylurea
    • Used to treat type II diabetes
    • Stimulates insulin secretion by blocking K+ATP channels in B cells
    • Require functioning B cells
    • Also block other K+ATP channels e.g. vascular smooth muscle
    • T1/2 = 4h - favoured
    • Side effects: hypoglycaemia, stimulate appetite, drug interactions (NSAIDs, warfarin, antifungals)
  174. Chlorpropamide
    • Sulphonylurea
    • Used to treat type II diabetes
    • Stimulates insulin secretion by blocking K+ATP channels in B cells
    • Require functioning B cells
    • Also block other K+ATP channels e.g. vascular smooth muscle
    • T1/2 = 36h
    • Side effects: hypoglycaemia, stimulate appetite, drug interactions (NSAIDs, warfarin, antifungals)
    • Inhibits alcohol metabolism
  175. Repaglinide
    • Non-sulphonyl structures
    • Treats type II diabetes
    • Stimulate insulin secretion by blocking K+ATP channels in B cells
    • Require functioning B cells
    • Unknown if this is the same site as sulphonylureas
    • Relatively selective for B cells - reduced side effects?
  176. Nateglinide
    • Non-sulphonyl structures
    • Treats type II diabetes
    • Stimulate insulin secretion by blocking K+ATP channels in B cells
    • Require functioning B cells
    • Unknown if this is the same site as sulphonylureas
    • Relatively selective for B cells - reduced side effects?
  177. Rimonobant
    • Cannabinoid receptor antagonist
    • Developed to treat obesity
    • Causes increased insulin senstivity?
    • Recently withdrawn
  178. Exenatide
    • Treats type II diabetes as adjunct
    • Mimics incretin: acts through GLP-1 receptor
    • - increases insulin release
    • - inhibits glucagon release
    • - reduces blood glucose
    • Little risk of hypoglycaemia
    • Given only by s/c injection
  179. Diazoxide
    • Treats chronic hypoglycaemia
    • Non-diuretic thiazide structure
    • Promotes K+ATP channel opening
    • - blocks insulin release
    • Side effects: hypotension, reflex tachycardia
  180. Carbimazole
    • Thioureylene
    • Competitive inhibition of thyroperoxidase enzymes
    • - reduce iodination of tyrosine
    • - reduce T3 and T4 output
    • Treats hyperthyroidism
    • Slow reponse - relapse common
    • Side effects; hypothyroidism, skin rash (less common than carbimazole), granulocytopenia

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