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PBL > Drugs > Flashcards

Drugs Flashcards

1
Q

Acetylcholine esterase inhibitors

A

Useful in alzhiemers patients to increase electrical activity in the brain
Prevents the break down of Ach into choline and acetate.
Increases neuronal transmission by increasing the level and duration of neural transmission

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2
Q

Adalimumab

A

Monoclonal antibody
Inhibits the effects of TNFa, prevents binding to p55 and p57 receptors.
Decreases leukocyte migration, decreases epidermal thickness, causes apoptosis in cells with TNF aplpah receptors, inhibits the release of IL-6 and acute phase proteins.
Useful in decreasing inflammation such as in rheumatoid arthiritis

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3
Q

Adenosine

A

Used to decrease HR
Binds to A1 receptors on the heart, this is an inhibitory GPCR, inactivates adenylate cyclase reducing cAMP production this decreases calcium ion influx and increase postassium ion efflux leads to decrease action potential generation in conductile cells
Binds to A2 receptors - antagonist of wake signals
Binds to A2a receptors - agonist of sleep
A2 and A2a are found in the brain

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4
Q

Amoxicillin

A

Is a beta lactam antibiotic
Beta lactam ring mimics D-Ala-D-Ala
Binds to PBP transpeptidase enzyme, inhibits this.
Prevents crosslinking of proteoglycan in bacterial cell walls
Leads to death by osmotic burst as cell wall integrity reduced

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5
Q

Anthracycline

A

End in rubicin
Used in chemotherapy - is a cytotoxic non-specific antibiotic
Intercalated into DNA to destabilise DNA structures, causing DNA breakages, this alters the transcriptomes of the cell and can activate apoptosis if damage accumulates
inhibit topoisomerases 2 enzymes, leading to supercoiling and DNA tangles - unable to be transcribed leading to apoptosis.
Also metabolised into free oxygen radicals leading to DNA damage

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6
Q

Asparaginase

A

Is an induction chemotherapy drug
Acts in the ECF, hydrolyses asparagine to aspartic acid and ammonia.
Tumour cells are dependent of asparagine from the interstitial space, have no intracellular asparagine synthase.
When low supply of essential asparagine as no more in interstisial space, unable to produce protein leading to cell death
Self cells are not affected as contain in intracellular asparinge synthase so are able to produce their own asparagine
Asparagine is a non essential amino acid.
However some rapidly dividing cells such as rbcs can show lower levels of dependence on asparagine in the ECF

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7
Q

Aspirin

A

Is an NSAID
Inhibits COx-1 and Cox-2, prevents conversion of arachidonic acid into prostanoids
Is slightly selective for COX-1, this reduces the amount of thromboxane, this inhibts platelett aggregation
Also reduces prostaglandinds, which can help resolve pain,fever and inflammation, particularly by cox-2 inhibition reducing PE2 and PI2
Used as preventitive medication after a TIA

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8
Q

Atorvastatin

A

Is an antielempic
Acts on herpatocytes
inhibits HMG-CoA reductase enzyme, this reduces the production of myalonic acid a precursor for LDL
This prevents hepatocytes from synthesising cholesterol
Also increases the number of LDL receptors on hepatocytes so takes in more LDL.
This reduces the amount of LDL ‘bad cholesterol’ in systemic circulation.
This imporves cardiovascular health, reduces risk of a heart attack or stroke

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9
Q

Azithromycin

A

Is a macrolide
Is an antibiotic
Inhibits the 23sRNA of the 50s subunit on a bacterial ribosome.
Inhibits translocation of aminoacyl tRNA
This prevents protein elongation, Inhibits translocation leading to no protein production and cell death
Given to treat Chlamydia

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10
Q

Benzylpenicillin

A

Used to treat bacterial meningitis in over 16yrs
Is a beta lactam antibiotic
Beta lactam ring mimics D-Ala-D-Ala
Binds to PBP tranverse peptidase, inhibits this.
Prevents crosslinking of proteoglycan in bacterial cell walls
Leads to death by osmotic burst as cell wall intergiry reduced

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11
Q

Champix

A

Medication to help stop smoking, was previously available on the NHS but has now been withdrawn.
partial agonsit of alpha-4 beta-2 nicotinic acetylcholine receptors - has lesser effects than nicotine whilst preventing nicotine from binding
Helps ease withdrawal symptoms whilst reducing cravings

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12
Q

Chondroitin

A

Used in osteoarthiritis
Is a component of cartilage ECM
Thought to encourage collagen regneration
Inhibits cox-2 preventing inflammation and inhibits NO synthesis reducing cartilage damage
Is not recommended by NICE guidelines

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13
Q

Citalopram

A

Is an SSRI antidepressant
Inhibits SERT
This prevents the reuptake of seratonin from the synpatic cleft into the pre-synpatic neurone
This increases the concentration fo seratonin in the synpatic cleft so more likley to bind to a seratonin receptor on the post synaptic membrane - this increases the intensity and duration of synaptic signalling
This is thought to decrease depression based on the monoamine hypothesis of depression

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14
Q

Co-amoxiclav

A

Used for gram negative bacteria that produce beta lactamases
Cluvanic acid - is weaker bl than amoxacillin so is used as a suicide substrate
amoxacillin then follows the normal mechanism of action of beta lactams

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15
Q

Dexamethasone

A

Is a glucorticoid
Hydrophobic so difuses straight across the cell membrane
Binds to glucorticoid receptor in the cytoplasm, receptor is dimerised to be activated
Travel to nucleus to act as a transcription factor, alters gene expression
Reduces: vascular permeability, neutrophil migration, pro-inflammatory cytokines
Increases: anti-inflammatory cytokines, apoptosis of lymphocytes

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16
Q

Diclofinac

A

non-selective NSAID

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17
Q

Donepezil

A

Acetylcholineesterase inhibitor
Used in alzhimers treatment

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18
Q

Entonox

A

Gas and air - given for pain relief during pregnancy
High flow oxygen - encourages endorphin release
Nitrous oxides - partial agonist of opioid receptors.

Reduces mild pain, may cause hallucination and nausea

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19
Q

Fluoxotine (prozac)

A

SSRI

20
Q

Glucosamine

A

Used in osteoarthiritis
Thought to encourage cartilage regneration
Is a precursor for componenet of cartilage, glucosaminoglycans in the ECM.
Reduce NFKb and INFy signalling leading to less inflammation
Is not recommended by NICE

21
Q

Hyaluronic acid injections

A

Glycosaminoglycan - component of ECM
Acts as a lubricant and shock absorber reducing the burden and friction on cartilage to prevent damage.
Antioxidative, anti-inflammatory and analgesic effects.
Reduce pain and inflammation when injected into the synovium.
Can be bound to be aggrecan, increases the water content and viscotity of the synovial fluid.
Used to decrease pain and increase mobility in OA

22
Q

Ibuporfen

A

non-selective NSAID

23
Q

Infliximab

A

Monoclonal antibody
TNFalpha inhibitor, prevents interaction with p55 and p57 receptors

24
Q

Iron supplement

A

Taken orally absorbed into blood stream,
Aids Hb metabolism in the bone marrow
Reduce aneamia

25
Q

Lansoprazole

A

PPI
Oral
pro-drug: able to pass through membranes as uncharged
Attracted to acidic area around parietal cells as basic
Sulfoxide to sulfenic acid, is now charged so not able to pass through the membrane, leads to an accumulation/high conc of drug trapped in the canaliculi of the parietal cell.
Disulfide bond with cystene amino acid in proton pump - this is a covalent change so irreversible
Conformational change inhibits the proton pump
Reduces H+ conc in stomach
Used to prevent acid reflux.

26
Q

Bupivacaine (epidural)

A

Nerve block from T10 to L1 space
No sensation below level of block
Used in pregnancy - only administered by an anesthesiologist
Blocks voltage gated sodium ion channels.

Side effects: prolonged labour

27
Q

Mercaptopurine

A

Is a maintenance chemotherapy drug.
Pro-drug
Converted to TIMP inhibits processes involving IMP this inhibits purine synthesis
Converted to TGTP - inserted into RNA to prevent elongation
Converted to TdGTP - inserted into DNA to prevent semi-conservative replication
This inhibits the S stage of interphase, preferntially affects rapidly dividng cells.

28
Q

Metformin

A

Is an anti-hyperglycemic
Enters hepatocytes by OTC-1 channel
Inhibits mitochondrial complex 1 - reduces ATP production
AMP?ADP: ATP ratio increases
Activates AMPKA
This inhibits fructose-1,6-biphosphate enzyme.
This inhibits gluconeogenesis and promotes glycolysis.
Also inhibits acetyl-CoA carboxylase inhibitng fat synthesis

Also increases cell sensitivity to insulin
Decreases glucose absorption in enteroendocytes in the SI
This leads to decreased blood glucose - reduces risk to bv in type 2 diabetics

29
Q

Methotrexate

A

Is an anti-folate (anti-metabolite) used as an induction chemotherapy drug
Inhibitis Dihydrofolate reductase, this prevents the conversion of dihydrofolate into terthydrofolate
This inhibits thymine synthesis, inhibits DNA and protein production.
Also inhibits AICART (purine synthesis), increased levels of AICAR have anti-inflammatory effects
Results in cell death
Preferentially targets rapidly dividing cells

30
Q

Metronidazole

A

Antimicrobial for anaerobic bacteria and parasites - typically used against a C.Diff infection
The nitro group is reduced the ferrodoxin or falvodoxin enzyme only found in target organism
This creates free nitrile radicals that are able to bind to and oxide DNA
This damages DNA, prevents DNA replication and has cidal acitivity

31
Q

Naproxen

A

NSAID

32
Q

Omeprazole

A

PPI

33
Q

Oseltamivir

A

Inhibits neuraminidase catalysed cleavage
Prevents influenza viruses from leaving the infected host cell

34
Q

Oxytocin

A

Used to induce labour or prevent pph and the mothering hormone
Negative feedback to reduce levels of progesterone
Binds to receptors to trigger/strengthen uterine muscle contractions, by increasing intracellular calcium in uterine myofibrils.
Increased by positive feedback until parturition finshed
Is also produced naturally by the body, concerns that may cause too fast labour

35
Q

Paracetamol

A

NSAID
Acts centrally not peripherally
Thought to inhibit cox-3 preventing conversion of arachadonic acid into prostanoids.
INhibits Cox1 and cox2 to increase the pain threshold
Leads to reduced fever and pain.
Exact mechanism is unknown

36
Q

Pethidine

A

Intramuscular Opiod used to relieve pain during labour
Binds to receptor on presynaptic neurone - inhibitor GPCR prevents calcium ion influx
Binds to receptor on postsytnaptic neurone - activatory GPCR leads to increase K+ efflux
Results in hyperpolarisation of membrane
Reduces the probability of an action potential being triggered, closes the pain gate

37
Q

Picolax

A

Laxative - used to clear the bowel before colonectomy.
Contains sodium picosulfate and magneisum citrate which are converted into active forms by sulfatases in the gut
Increases water secretion and inhibits electrolye and water absorption
Increases peristalsis of the colon - faster expulsion of more watery stools.

38
Q

PrEP

A

Used to prevent HIV infection
Typically contains tenofovir - inhibits reverse transcriptase
Emtricitabine - reverse trasncriptase
Creates a protective barrier around lymphocytes to stop from being invaded by HIV particles and prevents HIV from replicating
Must be taken daily and before HIV infection occurs
Is a preventative medication

39
Q

Propranolol

A

Is a beta blocker
Antagonist of beta adrenergic receptors
B1 - inhibiting decrease heart rate
B2 - inhibiting causes vasodilation
B2 in lungs, inhibitng can cause bronchspasm, therefore not given to asthmatics of COPD patients as unable to dilate
Is a structural analogue of adrenaline
Inhibits adenylate cyclase - reducing intracellular calcium so reduces muscle contractility.

40
Q

Thrombolysis

A

Medication to beak down blood clots
Alteplase - is a human made form of a plasminogen activator.
Binds to fibrin and plasminogen, converts plasminogen to plasmin (fibrin is a catalyst)
Plasmin degrades the fibrin matrix of thrombus promoting dissolving of the clot.

41
Q

Vincristine

A

Is an induction chemotherapy treatment
Binds to beta tubulin, prevents dimerizing with alpha tubulin.
Unable to form the polymer component of microtubules
Spindle apparatus does not form
Mitosis inhibited at metaphase
Leads to cell death
Preferentially affects rapidly dividing cells.

42
Q

Zyban

A

Norepinehprine and dopmaine reuptake inhibitor (major depressive disorder and to aid smoking cesssation)
Inhibits NET and DAT
Interferes with dopamine reuptake in the reward pathway - reduce addiction
Acts as a low dose nicotine substitute
Antagonism of nicotinic acetycholinergic receptors

43
Q

Nitrominidazole

A

Nitroimidazole antimicrobials
nitro group is converted to active compound by enzymes only found in the target organism (ferrodoxin or falvodoxin)
Nitrile free radicals damage DNA - impedes DNA replication and activates apoptosis pathway
Anaerobic bacteria and parasites

44
Q

Rosehip extract

A

Contains polyphenols - increase endorphin production and act as an anti-toxin
Vitamin c - anti-toxin
Inhibits NF B signalling and decreases levels of CRP leading to reduced inflammation.

45
Q

Curcumin

A

Inhibits cox-2,
Inhibits NF-B signalling
reduces inflammatory mediators

46
Q

What are the three branches of prostanoid production?

A

Prostacyclin PGI2 : involved in vasodilation and decreases platelet aggregation
Thromboxane: causes platelet activation and vasoconstriction - can lead to a thrombus formation
Prostaglandins E2 and I2: Can lead to pain, inflammation and gastric protection.

PBL (23 decks)

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