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Year 2 semester 2 > Drugs > Flashcards

Drugs Flashcards

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1
Q

Interferons

A

Decreases proinflammatory cytokines
Increases antinflammatory cytokines
Inhibits entry of immune cells into the CNS
Interferes with T-cell adhesion to endothelium
Reduces T-cell activation by interfering with HLA class II molecules

Flu-like symptoms
Rash/necrosis at the site of injection
Cognitive changes e.g depression
Bone marrow failure

MS 1st line

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2
Q

Glatiramer acetate

A

Decoy protein for myelin basic protein

Flushing 
Rash
Chest tightness
Palpitation
Anxiety
Dyspnoea

MS 1st line (but after Interferons)

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3
Q

Natalizumab

A

Binds to alpha-4 integrins on CD52 T cells
Stops them binding to BBB

Hypersensitivity reaction, Develop neutralizing antibodies
MS 2nd line

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4
Q

Finglomod

A

Prevents progress of lypmhocytes from secondary lymphoid tissue

Slight Immunosuppression
MS 2nd Line

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5
Q

Mitoxantrone

A

Type II topoisomerase inhibitor
Prevents DNA transcription to RNA

Cardiotoxic
Max use 2-3 years
MS 3rd line

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6
Q

Methotrexate

A

Folate inhibitor
Immunosuppressant
MS 3rd line

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7
Q

Azathioprine

A

Purine analogue

Immunosuppressant

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8
Q

Glucocorticoids- methylprednisolone

A

Has anti-inflammatory and immunosuppressant effects. Affects both early and late stage inflammation. Decreases extravasation activation of neutrophils. Either: Upregulates expression of anti-inflammatory proteins in the nucleus or Represses the expression of proinflammatory in the cytosol.

Opportunistic infections
Sudden withdrawal can cause adrenal insufficiency, Cushing’s, osteoporosis, hyperglycaemia, depression and psychosis

MS Acute relapses

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9
Q

Analgesics: Paracetamol

A

Antipyretic , Weak COX inhibitor

1st line treatment for generalised headache

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10
Q

NSAIDS

A

COX inhibitors

Gastric problems

1st line treatment for generalised headache

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11
Q

Serotonin Agonists- Tryptans

A

Serotonin agonist
Block pain pathway
Inhibit vasoactive peptide release

Drowsiness

Severe Migraine 1st line

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12
Q

Serotonin Agonists- Ergots

A

Serotonin agonist

Worsening of nausea and vomiting
Rebound headaches

Severe migraine 2nd line

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13
Q

Beta adrenergic blocker: Propanolol

A

Beta adrenergic blocker

Bradycardia, Hypotension

Migraine prophylaxis

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14
Q

L-dopa: Levadopa

A

Dopamine precursor

Nausea/Vomiting
Hypertension
Psychosis
Long-term – Dyskinesia
Death

1st line PD, Usually given with COMT or decarboxylase

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15
Q

Dopamine receptor agonist: Bromocriptine (ergot)

A

Direct D2 agonist

Nausea
Postural hypertension
Sleep attacks (narcolepsy)
Chest and pulmonary problems

1st line PD, Not available on the PBS

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16
Q

Dopamine receptor agonist: Pramiprexol (non-ergot)

A

Direct D2-3 agonist

Nausea
Postural hypertension Sleep attacks narcolepsy)

Better tolerated than Bromocriptine

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17
Q

Monoamine oxidase inhibitor: Selegiline

A

Protects DA from degradation

Confusion
Delirium
Hypertension

2nd line PD, 4th line depression

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18
Q

Enzyme inhibitor: Decarboxylase inhibitor: Carbidopa

A

Protects L-dopa from degradation to dopamine in the peripheries

Confusion
Delirium

Adjunct 1st line for PD

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19
Q

Enzyme inhibitor: COMT

A

Reduces metabolism of L-dopa to 3-OMD Confusion , Delirium

Adjunct 1st line PD

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20
Q

Anticholinergenics: Benztropine, Benzhexone

A

Muscarinic receptor antagonist

Dry mouth
Nausea
Constipation
Palpitations
Arrhythmias

PD, Limited use for patients on antipsychotics

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21
Q

Antiviral: Amantadine

A

Increased release, inhibit reuptake, dopamine agonist , NMDA receptor antagonist

Less severe but similar to L-dopa

PD 2nd line (1st line for mild-moderate)

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22
Q

VMAT 2 Inhibitor: Terabenazine

A

Blocks DA transport into vesicles in presynaptic terminal, Depletes DA , Decreases dopamine transmission

Allergic reaction
Extreme drowsiness
Mood or behaviour changes 
Agitation
Tremor
Trouble swallowing
Dizziness or fainting

HD 1st line

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23
Q

Neruoleptics: Haloperidol, Risperidone, Olanzapine

A

HD 1st line (refer to antipsychotics)

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24
Q

GABA agonists: Baclofen

A

G-coupled receptor

Loss of muscle tone

HD 1st line

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25
GABA Agonist: Clonazepam
Ionotropic receptor Tolerance Sedation Coma HD 1st line
26
Na+ channel blockers: Phenytoin, Carbamazapine, Lamotrigine, Primidone
``` Acts on sodium voltage gated channels Use dependent (Preferentially blocks neurons with higher activity) ``` Acne Teratogenic Hirsuitism Hormone imbalances Epilepsy Focal seizures – 1st line Carbamazapine Acute bipolar (mania) Grand Mal – lamotrogine
27
Ca2+ channel blockers: Ethosuxamide
T-type calcium channel blockers GIT Lethargy Nausea/Vomiting Absent seizures
28
Valproate
Decreases rate of slow sodium channels Decreased activity of t-type calcium channels Decreases GABA transaminase Increased GABA synthesis ``` GIT Fatigue Hair loss Tremor Rash ``` 1st line most seizures and Acute bipolar (mania)
29
Gabapentin
Sodium, calcium and GABA release Somnolence Dizziness 3rd line epilepsy
30
Topiramate
AMPA receptor on glutamate, sodium and Calcium Loss of cognitive function Dizziness Amnesia 3rd line epilepsy
31
GABA Potentiator: Vigobatrin
Inhibits transaminase Sedation Drowsiness Agression Psychosis (rarely) 2nd line epilepsy
32
GABA Potentiator: Benzodiazapines (Lorazepam, Diazepam, Clonazepam)
Increases frequency of CL channel opening Sedation Drowsiness Muscle relaxant Hypnotic 2nd line epilepsy, Anxiolytic 1st line acute panic attacks
33
GABA potentiator: Midazolam
Increases duration of Cl channel opening Sedation Drowsiness 2nd line epilepsy
34
GABA Potentiator: Barbituates (Phenobarbitol)
GABA-A cl- channel agonist, Increases duration of cl- opening Sedation Drowsiness 3rd line epilepsy
35
GABA Analogue: Acamprosate
Increases GABA, NMDA receptor inhibition Headaches Diarrhoea Pruritis (sometimes) Protracted withdrawal (not recommended for acute phase)
36
Enzyme blocker: Disulfiram
Blocks acetaldehyde dehydrogenase Hangovers Depression and psychotic symptoms Peripheral neuropathy Liver damage Adjunct for alcoholism
37
Opioid receptor antagonist: Naltrexone
Blocks (mu) opioid receptors Prominent nausea Headaches Dysphoria 1st line for alcoholism withdrawal
38
Monoamine inhibitors: Moclobemide, Selegiline
Inhibit MAO outside the mitochondria in the synaptic terminal ``` Significant hypertension when combined with tyramine Tremors Insomnia Convulsions Weight gain ``` 4th line for depression
39
Monoamine uptake inhibitors: SSRI (Sertraline Fluoxetine Paroxetine Citalopram Escitalopram)
Increase extracellular level of serotonin by inhibiting SERT ``` Headaches Dizziness Nausea Hyponatremia Serotonin Syndrome ``` 1st line depression 1st line pharmacological treatment for GAD, panic attacks, eating disorders, OCD
40
TCAs (Amitryptaline (tertiary amine) | Nortryptaline (secondary amine)
Inhibit reuptake of SERT and NET Anti-cholinergic Anti-histaminergic Anti-adrenergic 3rd line for depression
41
SNRIs (Venlaxafine, Desvenlaxafine)
Inhibit 5HT and NA reuptake SSRIs plus CV risk 2nd line for depression
42
NRI Reboxetine
Selective NET Less SSRI types but increase CV effects Insomnia 2nd line for depression
43
Atypical tetracyclics: Mianserin
Increases NA release by blocking alpha2 adrenoreceptors (autoreceptors), Inhibits uptake of NA Headache Drowsiness Fatigue Dry mouth
44
Atypical tetracyclics: Mirtazapine
Increases 5HT, NA release by blocking alpha2 adrenoreceptors and 5ht2 and 3 (autoreceptors) Headache Drowsiness Fatigue Dry mouth
45
Mood stabiliser: Lithium
Targets secondary messenger systems that modulate neurotransmitters Reduced excitatory eg. DA and Glut. Increases inhibitory eg. GABA ``` Restlessness/tremors Bloating Fluctuations of weight Acne Alopecia Depression ``` 1st line therapy bipolar disorder
46
Antipsychotics: Typical (Chlorpromazine, Haliperidol)
Strong antagonists of D2 and some D1 Weak antagonists at 5HT2 receptors Main effects against positive symptoms ``` Dystonia Parkinsonism Hyperprolactemia Akithesia Tardive dyskinesia ``` 2nd line for psychosis
47
Antipsychotics: Atypical (Respiridone, Clozapine, Olanzapine, Reserpine)
Weak D2 antagonists, Strong 5HT2 antagonists Efficacy against positive and negative symptoms Weight gain Agranulocytosis CVS risk ``` 1st line for: Acute and chronic psychosis Acute mania Organic psychosis Severe behavioural disorders in children Tourette’s Other choreas ```
48
Thyoid Hormone replacement: Levothyroxine
Acts as a T4 analogue which is partially converted to T3 Cardiovascular – palpitations, tachycardia, arrhythmias angina, cardiac arrest CNS – tremors, headache, nervousness insomnia, GI – diarrhoea, vomiting, Hypersensitvity, Weight loss, Menstrual irregularities, Sweating, Heat intolerance Treatment of choice in hypothyroidism
49
Beta Blockers: Propranolol
Relieves tachycardia, tremor, diaphoresis, anxiety No effect on underlying hormone secretion Used for symptomatic relief until hypothyroidism is resolved
50
Thioureas: Carbimazole and Propylthiouracil
Inhibits thyroid synthesis by concentrating in the thyroid gland and inhibiting the organic binding of I2. Inhibits iodination of tyrosine residues. ``` Headache Joint pain Rashes Pruritis GIT disturbances Alopecia Jaundice Myopathies Abnormal blood cells Agranulocytosis (within 60 days) Hyperthyroidism ``` Hyperthyroidism 1st line , Adjunct to radioactive iodine
51
Radiotherapy: Radioactive Iodine (131)
Taken up and processed the same was as normal iodine. Emits beta and gamma rays. The beta particles are absorbed by the tissue and has a powerful cytotoxic effect. This effect is restricted to thyroid follicle cells Hypothyroidism 1st line for hyperthyroidism
52
Insulin Sensitiser: Biguanides Metformin
Reduce hepatic glucose output through activation of enzyme of AMP activated protein kinase Increase glucose uptake by peripheries Mechanisms are unknown ``` Nausea Vomiting Abdominal discomfort Diarrhoea Weight loss ``` 1st line Diabetes type 2
53
Insulin sensitiser: Glitazones, Pioglitazone, rosiglitazone
Ligands of peroxisome proliferator activated receptor gamma (PPAR-g). Modulate expression of genes involved in lipid and glucose metabolism, insulin signal transduction, tissue differentiation. Increased lipogenesis ``` Fluid retention Immune system Increased risk of heart failure Loss of bone mineral density Weight gain ``` 3rd line Diabetes type 2. With continued metformin and insulin secretagogues
54
Insulin secretagogues: Sulfonylureas
Binds to ATP-sensitive potassium channels on the surface of pancreatic B-cells. Closure of the channel and depolarisation of the B cell Ca entry Insulin release Hypoglycaemia 1st line Diabetes Type 2, Only used in patients with some beta cell function
55
Insulin secretagogues: Meglitinides, repaglitinide
Modulate beta-cell insulin release by regulating potassium efflux through the same potassium channels as sulfonylureas Hypoglycaemia, Weight gain Greater effect on post-prandial increases in blood glucose than on fasting
56
Alpha glucosidase inhibitors: Acarbose, miglitol
Competitive inhibitor of alpha-glucosidase Mimimize upper intestinal digestion and defer digestion of the ingested starch 2nd line Diabetes type two With metformin and insulin secretagogue
57
Incretin enhancers
Inhibit the activity of dipeptidyl dipeptidase the enzyme that main enzyme that break downs GLP-1 and GIP. This inhibits secretion of the glucagon and inhibits gastric emptying and thus delays glucose absorption Headache Nausea Diarrhoea Increased rate of infections 2nd line Diabetes type 2 With metformin and insulin secretagogue
58
Amylin analogues: pramlitine
Supresses glucagon release Delays gastric emptying Adjuncts diabetes treatment
59
Adrenal enzyme inhibitors: Ketoconazole and aminoglutethimide
Inhibits cytochrome p450 enzymes P450scc and P450c11 Adjunctive therapy while in patients with mild disease while waiting for pituitary irradiation works
60
Adrenal steroidgenesis blockers: Metyrapone
Control hypersecretion of cortisol Adjunct therapy in treatment of Cushing’s syndrome
61
Adrenolytic: Mitotane
Adrenal atrophy predominantly in zona fasciculate and reticularis Severe nauseas Vomiting Diarrhoea Skin rashes
62
Adrenal replacement therapy: Corticosteriods (hydrocortisone)
Acts to replace cortisol
63
Mineralocorticoid supplements: fludrocortisones
Acts to replace aldosterone
64
Biphosphonates: Alendronate, risedronate
Inhibit osteoclast induced bone resorption, Increase bone density, Reduce incidence of fractures Nausea Chest pain Hoarseness Osteoporosis

Year 2 semester 2 (10 decks)

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