Drugs Flashcards
Interferons
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
Glatiramer acetate
Decoy protein for myelin basic protein
Flushing Rash Chest tightness Palpitation Anxiety Dyspnoea
MS 1st line (but after Interferons)
Natalizumab
Binds to alpha-4 integrins on CD52 T cells
Stops them binding to BBB
Hypersensitivity reaction, Develop neutralizing antibodies
MS 2nd line
Finglomod
Prevents progress of lypmhocytes from secondary lymphoid tissue
Slight Immunosuppression
MS 2nd Line
Mitoxantrone
Type II topoisomerase inhibitor
Prevents DNA transcription to RNA
Cardiotoxic
Max use 2-3 years
MS 3rd line
Methotrexate
Folate inhibitor
Immunosuppressant
MS 3rd line
Azathioprine
Purine analogue
Immunosuppressant
Glucocorticoids- methylprednisolone
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
Analgesics: Paracetamol
Antipyretic , Weak COX inhibitor
1st line treatment for generalised headache
NSAIDS
COX inhibitors
Gastric problems
1st line treatment for generalised headache
Serotonin Agonists- Tryptans
Serotonin agonist
Block pain pathway
Inhibit vasoactive peptide release
Drowsiness
Severe Migraine 1st line
Serotonin Agonists- Ergots
Serotonin agonist
Worsening of nausea and vomiting
Rebound headaches
Severe migraine 2nd line
Beta adrenergic blocker: Propanolol
Beta adrenergic blocker
Bradycardia, Hypotension
Migraine prophylaxis
L-dopa: Levadopa
Dopamine precursor
Nausea/Vomiting Hypertension Psychosis Long-term – Dyskinesia Death
1st line PD, Usually given with COMT or decarboxylase
Dopamine receptor agonist: Bromocriptine (ergot)
Direct D2 agonist
Nausea
Postural hypertension
Sleep attacks (narcolepsy)
Chest and pulmonary problems
1st line PD, Not available on the PBS
Dopamine receptor agonist: Pramiprexol (non-ergot)
Direct D2-3 agonist
Nausea
Postural hypertension Sleep attacks narcolepsy)
Better tolerated than Bromocriptine
Monoamine oxidase inhibitor: Selegiline
Protects DA from degradation
Confusion
Delirium
Hypertension
2nd line PD, 4th line depression
Enzyme inhibitor: Decarboxylase inhibitor: Carbidopa
Protects L-dopa from degradation to dopamine in the peripheries
Confusion
Delirium
Adjunct 1st line for PD
Enzyme inhibitor: COMT
Reduces metabolism of L-dopa to 3-OMD Confusion , Delirium
Adjunct 1st line PD
Anticholinergenics: Benztropine, Benzhexone
Muscarinic receptor antagonist
Dry mouth Nausea Constipation Palpitations Arrhythmias
PD, Limited use for patients on antipsychotics
Antiviral: Amantadine
Increased release, inhibit reuptake, dopamine agonist , NMDA receptor antagonist
Less severe but similar to L-dopa
PD 2nd line (1st line for mild-moderate)
VMAT 2 Inhibitor: Terabenazine
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
Neruoleptics: Haloperidol, Risperidone, Olanzapine
HD 1st line (refer to antipsychotics)
GABA agonists: Baclofen
G-coupled receptor
Loss of muscle tone
HD 1st line
GABA Agonist: Clonazepam
Ionotropic receptor
Tolerance
Sedation
Coma
HD 1st line
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
Ca2+ channel blockers: Ethosuxamide
T-type calcium channel blockers
GIT
Lethargy
Nausea/Vomiting
Absent seizures
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)
Gabapentin
Sodium, calcium and GABA release
Somnolence
Dizziness
3rd line epilepsy
Topiramate
AMPA receptor on glutamate, sodium and Calcium
Loss of cognitive function
Dizziness
Amnesia
3rd line epilepsy
GABA Potentiator: Vigobatrin
Inhibits transaminase
Sedation
Drowsiness
Agression
Psychosis (rarely)
2nd line epilepsy
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
GABA potentiator: Midazolam
Increases duration of Cl channel opening
Sedation
Drowsiness
2nd line epilepsy
GABA Potentiator: Barbituates (Phenobarbitol)
GABA-A cl- channel agonist, Increases duration of cl- opening
Sedation
Drowsiness
3rd line epilepsy
GABA Analogue: Acamprosate
Increases GABA, NMDA receptor inhibition
Headaches
Diarrhoea
Pruritis (sometimes)
Protracted withdrawal (not recommended for acute phase)
Enzyme blocker: Disulfiram
Blocks acetaldehyde dehydrogenase
Hangovers
Depression and psychotic symptoms
Peripheral neuropathy
Liver damage
Adjunct for alcoholism
Opioid receptor antagonist: Naltrexone
Blocks (mu) opioid receptors
Prominent nausea
Headaches
Dysphoria
1st line for alcoholism withdrawal
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
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
TCAs (Amitryptaline (tertiary amine)
Nortryptaline (secondary amine)
Inhibit reuptake of SERT and NET
Anti-cholinergic
Anti-histaminergic
Anti-adrenergic
3rd line for depression
SNRIs (Venlaxafine, Desvenlaxafine)
Inhibit 5HT and NA reuptake
SSRIs plus CV risk
2nd line for depression
NRI Reboxetine
Selective NET
Less SSRI types but increase CV effects
Insomnia
2nd line for depression
Atypical tetracyclics: Mianserin
Increases NA release by blocking alpha2 adrenoreceptors (autoreceptors), Inhibits uptake of NA
Headache
Drowsiness
Fatigue
Dry mouth
Atypical tetracyclics: Mirtazapine
Increases 5HT, NA release by blocking alpha2 adrenoreceptors and 5ht2 and 3 (autoreceptors)
Headache
Drowsiness
Fatigue
Dry mouth
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
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
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
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
Beta Blockers: Propranolol
Relieves tachycardia, tremor, diaphoresis, anxiety No effect on underlying hormone secretion
Used for symptomatic relief until hypothyroidism is resolved
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
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
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
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
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
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
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
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
Amylin analogues: pramlitine
Supresses glucagon release
Delays gastric emptying
Adjuncts diabetes treatment
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
Adrenal steroidgenesis blockers: Metyrapone
Control hypersecretion of cortisol
Adjunct therapy in treatment of Cushing’s syndrome
Adrenolytic: Mitotane
Adrenal atrophy predominantly in zona fasciculate and reticularis
Severe nauseas
Vomiting
Diarrhoea
Skin rashes
Adrenal replacement therapy: Corticosteriods (hydrocortisone)
Acts to replace cortisol
Mineralocorticoid supplements: fludrocortisones
Acts to replace aldosterone
Biphosphonates: Alendronate, risedronate
Inhibit osteoclast induced bone resorption, Increase bone density, Reduce incidence of fractures
Nausea
Chest pain
Hoarseness
Osteoporosis
