DRUGS Flashcards

Question

Indomethacin

Answer 1

NSAID More COX1 selective Anti-inflammatory More adverse effects due to COX1 selectivity

Answer 2

NSAID analgesic and anti-inflammatory Fewer side effects

Answer 3

NSAID more potent than indomethacin Analgesic for inflammatory pain Adverse effects = GI and headaches

Answer 4

Analgesic + antipyretic but no anti-inflammatory Side effects: - liver toxicity - no GI effects

Answer 5

COX2 inhibitor | Has cardiac risk

Answer 6

``` Opioid High efficacy Mimics endogenous opioids (enkephalins) and acts on mu receptors = pain inhibitory system Used for acute and chronic pain Side effects: - euphoria - respiratory depression - decreased GI motility (constipation) - opioid dependence ```

Answer 7

``` Opioid Low efficacy - slow release = no euphoria Used for acute and chronic pain Side effects: - decreased GI motility - respiratory depression ```

Answer 8

``` Opioid High efficacy Used for reduction of heroin addiction Side effects: - decreased GI motility - respiratory depression ```

Answer 9

``` Opioid High efficacy Used for high powered pain relief Side effects: - decreased GI motility - respiratory depression ```

Answer 10

Preventers - corticosteroid e.g. inhaled fluticasone + oral prednisolone - leukotriene receptor blockers - B agonists LABA: salmeterol and SABA: salbutamol

Answer 11

Non-depolarising NMB | Can be reversed by acetylcholinesterase inhibitor e.g. neostigmine

Answer 12

Depolarising NMB

Answer 13

Spasmolytic - relax overactive muscles Acts on GABAa receptor (inhibitory neuron) CNS Used as a sleeping pill

Answer 14

Spasmolytic - relax overactive muscles Acts on GABAb receptors (inhibitor metabotropic) CNS

Answer 15

Spasmolytic - relax overactive muscles | Acts in periphery - reduces release of calcium from internal muscle cell stores

Answer 16

Spasmolytic - relax overactive muscles Acts in periphery - cut up SNARE proteins required for the release of ACh vesicles Used in cosmetics and to relieve painful muscle spasms such as Cervical Dystonia (head and neck)

Answer 17

Metabolic precursor of dopamine Given with dopa decarboxylase (Carbidopa) to prevent conversion to dopamine in the periphery = goes to the brain for conversion (dopamine can't cross BBB) Used as first line treatment for Parkinson's Disease Problems: - hallucinations + delusions - dyskinesia - on-off phenomenon (sudden, unpredictable movements) - decreased effectiveness due to cell death

Answer 18

Dopamine agonist Used in combination with L-dopa to smooth off on-off phenomenon Less effective but lasts longer and less risk of dyskinesia Given as sc injection Used as second line treatment for Parkinson's disease Side effects: - nausea/vomiting - hallucinations - dopamine + reward system = compulsive shoppers or gamblers

Answer 19

MAO inhibitor - Used in early stages - Helpful for treating anti-depressant effects in later stages COMT inhibitor both can be used in combination with L-dopa to increase its effectiveness Last line of treatment

Answer 20

Typical antipsychotic (1st gen) Dopamine type 2 receptor antagonist or inverse agonist Used in the treatment of Schizophrenia postive symptoms (hallucinations + delusions) Side effects: - Parkinson-like effects due to decreased dopamine in nigrastriatal pathway - induces negative side effects due to decreased dopamine in prefrontal cortex - wide spread side effects because affects other receptors in the body (muscarinic, histamine, alpha adrenergic)

Answer 21

Atypical antipsychotic (2nd gen) Interacts with D1 and D2 dopamine receptor types + blocks serotonin receptors (involved in increased dopamine activity) Less affinity for other receptors = less side effects that 1st gen Side effects: - less risk of Parkinson-like effects due to decreased dopamine in nigrastriatal pathway - less side effects due to muscarinic, histamine, alpha adrenergic receptor binding in rest of body More commonly used than 1st gen for the treatment of Schizophrenia positive symptoms

Answer 22

``` Benzodiazepines Positive Allosteric Modulators of GABAa receptors Benefits: - fast acting = no therapeutic delay - large TI (safe in overdose) - effective antagonist: Flumazenil ``` Diazepam has a long duration (24-48 hours) and used for short term relief of anxiety Alprazolam is medium duration and used for anxiety and depression Side effects: - drowsiness, confusion, amnesia, impaired coordination - can produce substantial impairment in everyday life problems: - problems in elderly due to accumulation (long plasma half-life) - tolerance: receptor desensitisation - dependence: withdrawal symptoms if stopped suddenly = increased anxiety first line treatment for acute anxiety (short term use <4 weeks)

Answer 23

partial agonist of 5HT (serotonin) receptors only clinically approved drug of its class for the treatment of anxiety side effects: - dizziness, headache, nervousness, light-headedness, nausea - side effects subside over time or with decreased dose safer long-term than BZDs: - no withdrawal symptoms - no tolerance or dependence - non-sedating so safer in overdose second line treatment if antidepressants don't work (only for GAD)

Answer 24

SSRIs (selective serotonin receptor inhibitor) and SNRIs (selective noradrenaline receptor inhibitor) Also tricyclic antidepressants (TCAs) More neurotransmitter in synapse = more binding to receptor Side effects: - anxiety, insomnia, fatigue, nausea, dizziness, palpitations - withdrawal syndrome with sudden discontinuation (milder than with BZD) side effects and therapeutic lag can be overcome with adjunctive BZD use for first 1-2 weeks first line treatment for chronic anxiety because wide range of effectiveness over many anxiety disorder types

Answer 25

Gaseous anaesthetics

Answer 26

1 - once induced administer gaseous anaesthetic at MAC 2. more lipid soluble = more potent 3. some gases act in synergy = both lower than MAC

Answer 27

1. water solubility high water solubility = slow delivery to CNS lipids low water solubility = fast delivery to CNS lipids 2. rate of ventilation high rate = more efficient gas delivery 3. partial pressure of gas high concentration = increased delivery 4. cardiac output high HR = high CO = more deliver to brain

Answer 28

Barbiturate = IV anaesthetic highly lipid soluble = fast onset + short duration Side effects: - reduced CO - hypotension - respiratory depression - reduced cerebral blood flow and O2 distribution

Answer 29

``` IV anaesthetic Disconnects thalamus from cortex = sensations to thalamus not processed by patient Very lipid soluble = fast onset + short duration Side effects: - amnesia - analgesia - rigidity - catatonia - disorientation + hallucinations ```

Answer 30

Local anaesthetic Blocks VSSCs from inside the cell especially small diameter pain fibres (no myelin) = no depolarisation Use dependence (little goes via non-use-dependence pathway) Features of 'ideal local anaesthetic': - selective blockage of sensation - rapid onset + rapid reversibility - non-toxic systemically and locally

Answer 31

administer insulin rapid acting: Novorapid short acting: Actrapid long acting: Humulin NPH

Answer 32

Minimum choice protocol: - strict diet and exercise - no compensation for cheating - little flexibility - minimal decision-making - good blood glucose stability + minimal risk of hypoglycaemia Tight protocol: - patient wants to be proactive and self-managing - maintain optimal blood glucose levels - consists of 2 parts: maintain basal levels + adjustments for meals - - patient continuously monitors and adjusts - greater chance of hypoglycaemia

Answer 33

1st line treatment for type 2 diabetes Effects: - reduced glucose absorption in GIT - reduced gluconeogenesis in liver - increased insulin receptor sensitivity due to reduction in plasma insulin levels = increased glucose uptake + decreased hyperglycaemia Side effects: - diarrhoea + abdominal discomfort - contraindicated for patients with renal disease = accumulation + increased toxicity - lactic acidosis = lactate buildup in muscles

Answer 34

Weak bases that neutralise acids to form salt and water e.g. CaCO3, Mg(OH)2, Al2(OH)3 Used in mild cases of GORD - doesnt prevent over-production of acid Adverse effects: - excessive use of calcium salts = kidney stones - aluminium + calcium = constipation - magnesium = diarrhoea - calcium carbonate = produces gas and belching

Answer 35

Histamine (H2) antagonists H2 is GsPCR and causes increased gastric acid secretion Used in treatment of mild peptic ulcer + mild GORD Adverse effects: (usually minor) - headache - dizziness - diarrhoea - muscular pain - abrupt withdrawal = transient increase in gastric acid secretion = relapse of peptic ulcer/GORD

Answer 36

Proton Pump Inhibitor Covalently binds to proton pump (H+/K+ ATPase) = reduced basal and stimulated acid secretion Used as 1st line treatment for moderate to severe GORD or peptic ulcer (drug of choice for mild to severe gastric acid related disorders) Benefit of PPIs: - prolonged duration due to covalent binding - short plasma half-life Adverse effects: - headache - abdominal pain - nausea - caution in patients with hepatic disease because drug extensively metabolised - interferes with absorption of drugs that require acidic environment

Answer 37

Antiseptic Binds to -ve phosphates on lipid membrane on exterior of cells Prevents adherence and causes lysis at higher concentrations Specificity: targets all bacteria + affects our cells as well

Answer 38

Beta lactam Binds to PBP (penicillin binding protein) on transpeptidase which is involved in peptidoglycan cross-linking Bacteriocidal = creates holes in cell wall Specificity: gram +ve bacteria Low TI because human cells do not produce peptidoglycan

Answer 39

Aminoglycoside Irreversibly binds to 30S subunit of bacterial ribosome Specificity: gram +ve and gram -ve bacteria (not anaerobes as oxygen required in drug transport) low TI because some people have mitochondiral ribosomes that are very similar to bacteria = more susceptible to cell damage