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Semester 4 > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Co - Amoxiclav

  • class
  • indication
  • MoA
  • Side effects
A

Class - amoxicillin, beta lactate antibiotic
Indication - aspiration pneumonia, RTIs, UTIs.
MoA - inhibits formation of peptidoglycan cross links in bacterial cell wall, claculanic acid prevents survival of lactamase producing bacteria increase efficacy against resistance
- side effects - nausea, vomiting diarrhea, rash

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2
Q

Furosemide

  • indication
  • MoA
A

Acts on the thick ascending limb of the loop. It inhibits the NKCC1 transporter by attaching to the chloride binding site. These ions (sodium, potassium, chloride) cannot be reabsorbed. Therefore renal medulla is not made hypertonic, water remains in the collecting duct. Magnesium and calcium are lost in urine
- oedema, resistant, hypertension

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3
Q

What are the side effects of furosemide?

A
  • mild GI disturbances
  • pancreatitis
  • hypotension
  • electrolyte disturbances
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4
Q

Ramipril

  • indication
  • mechanism of action
A
  • high blood pressure
  • oedema associated with heart failure, renal disease and liver disease

ACE inhibitor, prevents conversion of AI to AII by inhibiting ACE,it is a prodrug that is converted to ramiprilat in the liver and kidneys (mostly liver)

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5
Q

Bisoprolol

A
  • indication: heart failure, angina, hypertension
  • MoA: competitive cardio selective beta 1 antagonist, blocks beta receptors on the heart to lower heart rate and blood pressure, leads to less of a workload on the heart, prevents renin release somehow leading to vasodilation
  • side effects: higher dose may block beta 2 receptors in the bronchial and vascular smooth muscle which can lead to bronchospasms and vasodilation
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6
Q

Antacids

A
  • class: magnesium/aluminum salts
  • indication: dyspepsia
  • MoA: direct neutralisation of gastric acid
  • side effects: magnesium = laxative, aluminium = constipation
  • other: contraindicated for patients with renal insufficiency
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7
Q

Simvastatin/ atorvastatin

A
  • Class: statin
  • indication: hypercholesterolemia
  • MoA: pro-drug that is converted to beta delta dihydroxy acid which competes with HMG-CoA for HMG-CoA reductive, reducing levels of meyalonic acid, the precusor to cholesterol
  • side effects: myalgia, athralgia, GI problems
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8
Q

Alginate e.g. gaviscon

A
  • indication: GORD, peptic ulcers
  • MoA: derived from algae creates a foam barrier to coat the upper stomach, combined with magnesium and aluminium salts to make antacids
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9
Q

Bismuth

A
  • class: quadruple therapy agent
  • indication: H.pylori
  • MoA: H.pylori can only divide at above pH 5.5, antibiotics of triple therapy work best when HP is dividing, which PPIs help to do. PPIs wear off though. Bismuth blocks proton influx into HP so antibiotics can work when HP wears off
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10
Q

Esomeprazole

A
  • Class: PPI
  • Indication: H.pylori
  • MoA: same as omeprazole but isn’t a mixture of the optic isomer,, it is only the S isomer which works better
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11
Q

Clarithromycin

A
  • Class: macrolide antibiotic
  • Indication: can be used in triple therapy
  • MoA: binds to 50s ribosomal subunit to stop protein synthesis in bacteria
  • NB: used if penicillin allergy is present
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12
Q

Cimetidine

A
  • Class: H2 receptor antagonists
  • Indication: gastric/duodenal ulcers, where gastric acid reduction is beneficial e.g. chronic pancreatitis
  • Inhibition of H2 receptor prevents histamine stimulating parietal cells to produce gastric acid
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13
Q

Pancreatin

A
  • Indication: chronic pancreatitis, system fibrosis
  • MoA: Mixture of enzymes produced by exocrine pancreas e.g amylase, lipase and trypsin
  • Side effects: soreness of personal skin, buffalo mucosa and perianal skin, GI disturbances
  • NB: soreness occurs if tablet is held in mouth or dosage is too high due to enzyme activity
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14
Q

Orlistat

Lower dose is called alistart

A
  • Class: lipase inhibitor
  • Indicator: obesity
  • MoA: Inhibits pancreatic lipase which breaks down triglycerides this reduces fat absorption by 30%
  • side effects: oily spots, flatulence, oily stools, vitamin absorption affected as some are fat soluble A,D,E,K
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15
Q

Fluorouracil

A
  • Class: pyramiding analog, thymidylate synthase inhibitor, antimetabolite
  • Indication- CRC
  • MoA: prevents pyramiding from incorporating into DNA during S phase, drug is converted to a fraudulent nucleotide called FDUMP and inhibits thymidylate synthase, preventing the conversion of 2 - deoxyuridylate DUMP to 2 - deoxythymidylate DTMP resulting in a decrease in DNA synthesis = cell death
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16
Q

Folinic acid

A
  • Class: calcium/sodium folinate
    -Indication: enhances the effect of fluorouracil, counteract cytotoxic drug methotrexate
    MoA: increases tetrahydrofolate for fluorouracil to bind with and increase stability of fluorouracil, thymidylate synthase complex = increase in cytotoxicity
    Side effects: rarely Pyrexia, insomnia, depression, agitation after increase in doses
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17
Q

Oxaliplatin

A

Class: chemotherapy drug
Indication: colorectal cancer
MoA: selectively inhibits DNA synthesis, converted to active derivatives that bind to macromolecules, after activation, preferentially binds to guanine and cytosine groups. This inhibits DNA synthesis and transcription
Side effects: OD, dyspnoea, wheezing, neuropathy, neutropenia, diarrhoea, Emeli’s, fatigue

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18
Q

Citalopram

A

Class: SSRI
Indication: depression
MoA: prevents uptake of serotonin leading to more serotonin being released at synapses
Side effects: enterochromaffin cells are found in the intestinal villi, they make serotonin, they act on vagus and ENS nerves on HT3 receptors, enterocytes have serotonin uptake transporters to remove it from the synapse. Therefore when SSRIs are used people get diarrhoea at first: impotence, drowsiness, nausea

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19
Q

Salbutamol/ ventolin

A
  • Class: Beta 2 antagonist
  • Indication: asthma, COPD
  • MoA: increases cAMP in bronchi smooth muscle
  • Side effects: tremors, headaches
20
Q

Hidrasec

A

Class: enkephalinase inhibitor
Indicators: diarrhoea
MoA: enkephalins are a group of endogenous opioids along with endomorphins. Normally PGE2 and secretin that work on GPCRs coupled with Gs stimulators that stimulates adenylate cyclise to make cAMP which stimulates the chloride channels. Enkephalins act on GPCRS primarily my that are coupled with Gi (inhibitory) proteins that inhibit adenylate cyclase

21
Q

Propranolol

A

Class: non selective beta blocker
Indication: hypertension, anxiety
MoA: blocks adrenaline and noradenaline at beta 1 and 2 adrenergic receptors
Side effects: bradycardia, heart failure

22
Q

Epcluza (sofosbuvir + velpatasvir)

A

Class: direct acting antivirals. NS5A inhibitor
Indication: hepatitis C/HCV
MoA: inhibit specific HCV non-structural proteins that are vital for replication

23
Q

Zepatier (Elbasvir + Grazoprevir)

A

Class: direct acting antivirals. NS5B inhibitor
Indication: hepatitis C/HCV
MoA: inhibit specific HCV non-structural proteins that are vital for replication

24
Q

Harmonica (sofosbuvir + Ledipasvir)

A

Class: direct acting antivirals. NS3/4A inhibitor
Indication: hepatitis C/HCV
MoA: inhibit specific HCV non-structural proteins that are vital for replication

25
Q

Pegylated interferon alpha 2a/2b and Beta 1a

A

Class: pegylated interferon
Indications: HCV, HBV, mutiple sclerosis
MoA: make interferons last longer to help cellular recognition of infection. Inhibits viral replication this way
Side effects: headache, tiredness, hair loss, fever

NB: typically added with ribavirin for HCV. Used to treat HBV but has port success rates - 25% but when it does work it destroys CCCDNA given for 48 weeks for HBV

26
Q

Ribavarin

A

Class: antiviral
Indication: HBV
Side effects: headache, tiredness, nausea, fever

NB: success depends on the genotype and degree of fibrosis, works best on genotypes 2 and 3 of HCV. With type 1, chance of cure is less than 50% with cirrhosis, chance of cure is 10%

27
Q

Tenofovir

A

Class: antiviral
Indication: HBV
MoA: nucleotide analogue that inhibits DNA polymerase: a key enzyme in HBV’s life cycle. This prevents further fibrosis

NB: must be taken lifelong and if stopped the DNA will replicate

28
Q

Entecavir

A

Class: antiviral
Indication: HBV
MoA: nucleoside analogue that inhibits DNA polymerase

NB: must be taken lifelong and if stopped the DNA will replicate

29
Q

Kava Kava

A

A Sedative used to treat anxiety. Proven by a Cochran’s review to be better than a placebo

Side effects: liver damage

30
Q

Insulin

A

Indications: diabetes
RA: 3 - 5 hours covers meal with injection
SA: 5 - 8 hours covers meals within 30 - 60 minutes
IA: 18 - 24 hours half a day/ full night used with RA/SA
LA: up to 24 hours full day with RA/SA
Pre mixed - taken 2/3 times a day before meals

31
Q

What are the side effects of using insulin?

A 
Hypoglycaemia 
Muscle wasting/pain at injection site 
Rarely allergic reaction 
Can be used in pregnancy 
Weight gain
32
Q

Metformin

A

Class: biguanide (insulin sensitiser)
Indications: first line drug for type II diabetes
MoA: Activates AMP kinase which is involved in GLUT4 metabolism and fatty acid oxidation, decrease in fluconeogenesisi in liver and increase in peripheral glucose uptake
Side effects: anorexia, epic Astrid discomfort, cramping

NB: only works if insulin is present therefore doesn’t work for T1DM

33
Q

Clotrimazole

A

Class: anti-fungal
Indication: otitis external, external candidiasis
Mechanism: alters fungal cell wall permeability by binding to the cell membrane phospholipids and inhibiting synthesis of cell membrane components
Side effects: itching, mild burning sensation

34
Q

Sulfonylureas

A

Class: insulin secretagogue
Indication: TII DM
MoA: activates sulfonylurea receptors which inhibits ATP sensitive potassium channels, increasing intracellular potassium leading to depolarisation and calcium influx leading to insulin release
Side effects: hypoglycaemia, weight gain, GI disturbances, increase beta cell destruction

35
Q

Rosiglitazone pioglitazone

A

Class: thiazolidinediones (Insulin sensitiser PPAR agonists)
Indication: TII DM
MoA: drug target is PPARgamma: peroxisome proliferator - activated receptor gamma. PPARgamma is a master regulator of adipocyte differentiation found on adipose cells. When PPARgamma is activated the receptor binds to DNA in complex with retinoid x receptors and increases fatty acid storage in adipocytes therefore decreasing fatty acid storage in adipocytes therefore decreasing FFA in blood. The drug activates PPARgamma to cause an increase in adipocyte differentiation, promoting glucose uptake by muscles.
Side effects: weight gain, oedema, no hypoglycaemia, osteoporosis

36
Q

DPP4 inhibitor

A

Class: insulin secretagogue
Indication: TIIDM
MoA: glucose dependent, increases insulin secretion, decreases glucagon secretion. DDP4 breaks down endogenous GLP1. Inhibiting DPP4 means more GLP1, GLP1 has receptors on beta cells and activation causes insulin release. Has same effects as GLP-1RAs: satiety and weight loss, slowed gastric emptying
Side effects: not used in pregnancy, no hypoglycaemia, urticarial, angioedema, weight loss

37
Q

GLP-1 receptor agonist

A

Class: glucagon like peptide, insulin’s secretagogue
Indication:T2DM
MoA: GLP1 receptor found on pancreas beta cells, activation stimulates ardently cyclise pathway leading to insulin release. Slows gastric emptying which increases satiety.
Side effects: less risk of hypoglycaemia than older insulin secretagogues, not used in pregnancy, GI side effects

38
Q

Alfa-interferon

A

Class: antiviral
Indication: chronic Hep B/C, cancer
MoA: proteins that interfere with viral replication and activate other immune cells
Side effects: flu-like symptoms, ocular effects, depression

39
Q

Trimethoprim

A

Class: antibiotic
Indication: UTIs
MoA: blocks folate metabolism in bacteria resulting in death
Side effects: nausea, rash, changes in taste

40
Q

Losartan

A

Class: A II receptor antagonist
Indication: hypertension
MoA: decreased peripheral resistance/after-load and cardiac venous return/preload
Side effects: foetal toxicity, upper respiratory infections, back pain, hyperkalaemia

41
Q

Aliskiren

A

Class: direct renin inhibitor
Indication: primary hypertension
MoA: renin cleaves angiotensinogen to A I, the drug binds to the S3 binding site of renin which is essential for renin to work
Side effects: hyperkaelmia, low BP, diarrhoea, angioedema

42
Q

Finasteride

A

Class: 5 alpha reductive inhibitor (selective for type II)
Indication: BPH, male pattern baldness
MoA: prevents metabolism of testosterone into dihydrotestosterone which is indicated in causing prostate enlargement
Side effects: impotence, decrease in libido, ejaculation disorders

43
Q

Dutasteride

A

Class: 5 alpha reductive inhibitor (selective for type l and II)
Indication: BPH, male pattern baldness
MoA: prevents metabolism of testosterone into dihydrotestosterone which is indicated in causing prostate enlargement
Side effects: impotence, decrease in libido, ejaculation disorders

44
Q

Tamsulosin

Alfuzosin

A

Class: alpha 1 blockers (tamsulosin selective for alpha 1a subtype specific to bladder/neck/prostate urethra)
Indication: BPH, kidney stones
MoA: inhibit the alpha 1/1a receptors resulting in relaxation muscles of bladder neck increase urinary flow and decrease in pain
Side effects: drowsiness, postural hypotension, syncope, retrograde ejaculation

45
Q

Amlodapine

A

Indication: hypertension, angina
MoA: affects smooth muscles and cardiac muscles, integers with calcium ions moving through slow channels of active cell membranes
Side effects: nausea vomiting and dizziness in overdose, abdominal pain, headaches, palpitation

Semester 4 (15 decks)

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