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Case 1, Case 9, Case 8, Case 2, Case 12, Case 4, Case 7, Case 11 - Coggle…
Case 1
Vasodilators
Nitrates (SL/Transdermal)
Nitric Oxide Donor > Releasing NO by releasing nitrates with tissue > SH groups which increase cGMP leading to smooth muscle relaxation > Reduce blood to heart. Dilate coronary arteries, increase blood to heart.
GTN, isosorbide mono or dinitrate, Nitroprusside, Amyl Nitrite (Inhale)
Indication
Stable Angina and Unstable Angina
Acute and Chronic HF
Contraindication
Hypotensive Conditions
Hypovolemia
Aortic Stenosis - Further decrease blood flow to body
Adverse Effects
Postural Hypotension (due to venous pooling)
Throbbing Headache
Flushing
Tachycardia
Methemoglobinemia
Hydralazine (Oral/IV)
Direct Acting Smooth Muscle Relaxant causing vasodilation.
Indication
Short term or severe hypertension in pregnancy
Contraindication
Acute poryphyrias
SLE
Adverse Effects
Lupus Erythematosus
Headache, Nausea, Anorexia, Palpitations, Sweating and Flushing
Peripheral Neuropathy
Minoxidil
Opening or K+ channels in smooth muscle membranes of blood vessels. This causes cells to relax and widen > vasodilation.
Indication
Last Resort - Severe Hypertension, unresponsive to others
Adverse Effects
Tachycardia, Palpitations and Angina
Ankle Swelling
Hypertrichosis
Calcium Channel Blockers
Dihydropyridines (DHPs)
Increase HR. Block Ca2+ entry into smooth muscles > Vasodilation
NifeDIPINE, AmloDIPINE, FeloDIPINE
Indications
Hypertension
Non-DHPs (Oral)
Benxothiazepines
Mixed vascular and cardiac effects.
Diltiazem
Phenylalkylamine
Predominantly cardiac effects
Verapamil
Decreases HR. Acts on L type voltage sensitive Ca2+ channels. Blocks Ca influx via L type Ca2+ channels. Slows depolarization in SA and AV node, slowing HR. T types are mostly found in the brain - seizures
Indications
Arrhythmias
Contraindications
Cardiogenic Shock
Adverse Effects
Flushing, Headache
Ankle Swelling
Reflex Tachycardia
Bradycardia + Heart Blocks (Non-DHPs)
Constipation, HF
Gingival Hyperplasia (DHPs)
Diuretics (Oral)
Reduce Blood Volume > Decrease SV > Decrease CO
Thiazides (Oral)
Hydrochlorothiazide
Bendroflumethiazide
Loop Diuretics (Oral/IV when urgent)
Furosemide
Bumetanide
Ethacrynic Acid
Indications
Severe oEdematous States
Potassium-Sparing Diuretics
Aldosterone-independent
Amiloride
Triamterene
Blocks the ENaC in the same portion of the nephron
Aldosterone Antagonists
Spirinolactone, Eplerenone
Competitive Antagonist of Aldosterone. Inhibits aldosterone-induced production of sodium transport proteins at collecting tubules > Reduce expression of genes that code for ENaC and Na+/K+ ATPase
Adverse Effects
Gynecomastia
Hyperkalemia
Hyponatremia
GI Disturbances
Indications
Hypertension
CHF
Adverse Effects
Hypovolaemia - Dehydrated, Dizzy
Electrolyte Imbalance
Hyperuricaemia - Kidney Stones
Mostly Thiazide
Hyperglycaemia
Thiazide
Sympatholytic Agents
Alpha 1 Adrenoreceptor Antagonists (Alpha Blockers)
Blocks Alpha 1 in smooth muscles > Vasodilation
Blocks Alpha 1 in Baroreceptors > Decrease baroreceptor sensitivity >Tachycardia
Relax urinary bladder neck and prostate > Promote Urinary Outflow
PraZOSIN, DoxaZOSIN, TeraZOSIN
Adverse Effects
First Dose Phenomenon
Vasodilation - Dizziness, Palpitations and Headache
Decrease Vasoconstriction - Sexual Dysfunction
Vasodilation - Nasal Congestion
Vasodilation - Postural Hypotension
Tachycardia
Indication
Hypertension
BPH
Beta Blockers
Non-selective
PropranOLOL, SotaLOL
Can cross BBB - CNS SE
Blocks β receptor > Reduce the effect of adrenaline/noradrenaline > Decreases HR and myocardial contractility (prolong AV refractory period) > Inhibition of RAS > Decreases Renin > Decrease SVR. Inhibits peripheral conversion of T4 to T3 - deiodinase inhibitor.
Cardio-selective
MetoprOLOL, AtenOLOL, BisoprOLOL, EsmOLOL
Adverse Effects
Bronchospasm
Lethargy and Fatigue
Obscures Hypoglycemic Symptoms in DM - Reduces blood sugar so masks DM SE
CNS Depression
K-old
Exacerbates/precipitates acute HF
Reduce CO
Sexual Dysfunction - Reduced blood flow to genitals
Indication
Hypertension
Chronic HF
Tachyarrhythmia provoked by increases sympathetic activity
Angina or Previous MI
Prevent Recurrent SVTs
Reduce ventricular dysrhythmias following MI
Blocks symptoms of sympathetic activity from hyperthyroidism.
Contraindications
Asthma
COPD
Alpha and Beta Antagonists
Labetalol, Carvedilol, Nebivolol
Centrally Acting (Oral)
Acts on the brain by suppressing sympathetic outflow directly (Clonidine) or indirectly by acting as a false neurotransmitter (Methyldopa) >Reduces SNS activity,
Adverse Effects
Drowsiness/Sedation
Postural Hypotension
Anemia Hemolytic
Methyldopa
Indications
Hypertension in Pregnancy (Methyldopa)
Migraine (Clonidine)
Acts on RAS System
ACEI (Oral)
CaptoPRIL, EnalaPRIL, LisinoPRIL
Dilates blood vessels by inhibiting Angiotensin II. Inhibit degradation of bradykinin (relaxes smooth muscles). Reduces salt retention by decreasing aldosterone secretion.
Adverse Effects
Cough
Angioedema
Tongue Swelling
Uticaria
Anaphylaxis
Potassium Increase
Taste Changes
Orthostatic Hypotension
Pregnancy Effects
Rash or Renal Failure
Increase Renin
Low Angiotensin II
Indications
Hypertension (even DM)
HF
Contraindications
Pregnangy
Known Allergy
Hyperkalemia
Bilateral Renal Artery Stenosis
ARBs (Oral)
LoSARTAN, CandeSARTAN
Inhibit action of AII. Results in Vasodilation so decreases SNS activity.
Adverse Effects
Indications
Contraindications
Renin Inhibitors
Aliskiren
Inhibit renin > decreases Angiotensin II
Adverse Effects
Indication
Hypertension
Contraindication
Concomitant Treatment with ACEI or ARBs can aggravate adverse effects.
Case 9
Antidepressants
SSRI (1st Line) (Oral)
Enhance serotonin neurotransmission by blocking its reuptake into the presynaptic neuron.
Fluoxetine
Sertraline
CistaloPRAM
Indications
Antidepressants
Anxiety Disorders
Premature Ejaculation
GAD/Panic Disorder
Paroxetine
Contraindications
Children under 18
May cause ventricular arrhythmias with risk of SCD
SNRIs
Block the reuptake for serotonin and NA.
Venlafaxine
Duloxetine
Mirtazapine
Adverse Effects
Loss of Libido
Constipation
Dry Mouth
Tricyclic Antidepressants (TCA) (Oral)
Block the reuptake for serotonin and NA.
Competitive Antagonist for serotonin and NA reuptake transporter
Amitriptyline
ClomiPRAMINE
Adverse Effects
Dry Mouth
Blurred Vision
Constipation
Urinary Retention
Sexual Dysfunction
Postural Hypotension
Monoamine Oxidase Inhibitors (MAOIs)
Prevent the Breakdown of Serotonin and NA. If stopping other MAOI, other antidepressants should not be started for 2 weeks.
Phenelzine
Tranylcypromine
Indications
Prescribed when TCAs are unsuccessful.
Adverse Effects
Postural Hypotension
Cheese Reaction
Increases Apeitie - Weight Gain
Adverse Effects
Hyponatremia - Mostly Elderly - Drowsiness, Confusion or Convulsions
Suicidal Behavior - Suicidal thinking, self harm or hostility behavior.
Serotonin Syndrome - Occur during combination (SSRI + MAOI) - Neuromuscular hyperactivity (tremor, hyperreflexia, clonus, myoclonus, rigidity). Autonomic dysfunction (tachycardia, hypertension, hyperthemia, shivering, diarrhea)
Auto
Discontinuation Symptoms - Flu like symptoms, dizziness, headache, irritability, brain zaps.
Sedative Hypnotics
Benzodiazepines (Oral)
Long Acting
DiaZEPAM, FluraZEPAM
GABA receptor enhancer - Modify the structure of receptor - GABA ligand binds easier and allow more frequent Cl- influx. Enhance the activity of GABA, membrane hyperpolarization and further suppress the neuronal stimulation. Can cross BBB, placenta and breast milk.
Moderate Acting
NitraZEPAM
Short or Ultra Short Acting
MidaZOLAM, TemaZEPAM
Indications
Anxiolytic Effect - Severe Anxiety
Sedative/hypnotic Effect - Severe Disabling Insomnia
Anaesthetic Effect
Anticonvulsant
Adverse Effects
Impair Cognitive and Psychomotor Function
Drowsiness and Confusion
Anterograde Amnesia
Respiratory and CNS Depression
Tolerance, physical and psychological dependence.
Barbiturates
Phenobarbitone, Thiopentone
GABA receptor enhancer. Increases the channel opening duration, compared to BZD which increases the channel opening frequency.
Indications
Adverse Effects
Impair Cognitive and Psychomotor function
Respiratory and CNS suppression.
Tolerance, physical and psychological dependence.
Buspirone
Partial Serotonin Receptor Agonist
Indications
GAD only.
Adverse Effects
Less severe than BZD/SSRI.
Headache, Dizziness, Nausea, Tachycardia, GIT direstress
Z- Class Hypnotics (Oral)
New Generation GABA Enhancer. No anxiolytic, anticonvulsant or muscle relaxing effects.
Adverse Effects
Headache, Dizziness
CNS depressants - respiratory depression
Levothyroxine
Indications
Hypothyroidism (1st Line)
Contraindications (Start low and gradually increase)
Elderly
IHD
Adverse Effects
Hyperthyroidism
Myocardial Ischemia, Arrhythmias, HF
Hyperthyroidism
Inhibitors of Iodine Uptake
Perchlorate
Pertechnetate
Thiocyanate
Compete with iodine for the uptake into the thyroid gland follicular cell resulting in a decreased amount of iodide available for thyroid hormone synthesis.
Inhibitors of Organification and Hormone Release
Iodides
Inhibit conversion of Iodine to MIT-DIT-T3-T4
Indications
Hyperthyroid patients before thyroidectomy
Severe thyrotoxic crisis
Adverse Effects
Allergic Reactions (Iodinism)
Radioactive Iodine
Indication
Nodular Thyrotoxicosis
Contraindications
Pregnancy
Thionamides (Methimazole, Carbimazole, Propylthiouracil)
Inhibit conversion of Iodine to MIT-DIT-T3-T4
Propylthiouracil - Inhibit Type 1 Deiodinase resulting in inhibition of peripheral conversion of T4 to T3. Preferred in pregnancy.
Adverse Effects
Hypothyroidism
Goitre
Agranulocytosis
Skin Rashes and Pruritus
Arthralgia, Hepatitis
Carbimazole/Methimazole - Crosses the placenta and cause fetal hypothyroidism and goitre.
Neutropenia
Peripheral Thyroid Hormone Metabolism
Beta Blockers
Ipodate
Glucocorticoid
Liothyronine (Oral/IV)
Indications
Hypothyroidism
Adverse Effects
Iodine
Indications
Cretinism
Prevent Endemic Goitre
Case 8
Inhibit Protein Synthesis
Macrolides
Erythromycin, Clarithromycin
Chloramphenicol
Broad spectrum for specific infections.
Clindamycin
G(+), MRSA
Streptogramins
Linezolid
Aminoglycosides
Tetracyclines
Inhibit Cell Wall Synthesis
Penicillins
MethICILLIN
Beta-Lactam Antibiotics
Narrow Spectrum
Mostly Against Gram (+)ve
Benzylpenicillin
Beta Lactamase Restistant/Anti-Staphylococcal
Flucloxacillin
Sensitive Staphylococci
Broad Spectrum
Amoxicillin, Ampicillin
Against G(+) and (-). Not penicillinase-resistant.
Extended Spectrum
Ticarcillin
Most active against negative. Active against Pseudomonas.
Cephalosporins
Cephalexin (1st)
Cefuroxime (2nd)
Beta-Lactam Antibiotics
Ceftriaxone (3rd)
Cefipime (4th)
Ceftraroline, Ceftobiprole (5th)
Monobactams
Aztreonam
Beta-Lactam Antibiotics
Carbapenems
ImiPENEM
Beta-Lactam Antibiotics
Bacitracin
Vancomycin
Disrupts Cell Membranes
Polymyxin
Daptomycin
Disrupt the bacterial outer cell membrane altering cell membrane permeability. Active against (-), VRE, MRSA
Interfere with Metabolic Pathways
Sulfonamides
Trimethoprim
Inhibit Nucleic Acids
Case 2
Reduce Preload/Reduce Afterload
ACEI (Oral)
ARBs (Oral)
Beta Blockers
Vasodilators
Arrhythmias
Non-Specific Interventions (Bradyarrhythmia)
Atropine
Atropine prevents the parasympathetic effect of the vagus nerve on the heart (SAN and AVN). Atropine is a competitive inhibitor of ACh at muscarinic receptor. Muscarinic receptor antagonists therefore reduce GI motility.
Indications
Symptomatic Sinus Bradycardia
AV Block (1st Line)
Organophosphate Poisoning
Diarrhea
IBS
Adverse Effects
Tachycardia
Dry Mouth
Dilated Pupils, Blurred Vision
Hot, dry flushed skin
Fever
CNS changes
Urinary Retention
Isoproterenol
B1/B2 adrenoreceptor agonist > Positive Chronotropic Effect
Indications
Atrioventricular Block
Bradycardia
Adverse Effects
Palpitations
Arrhythmias
Tremors
Specific Interventions (Tachyarrhythmia)
Supraventricular
Beta Blockers
Class III (Amiodarone, Dofetilide, Sotalol) - First line for ventricular fibrillation
Blocks K+ channels inhibiting Phase 3 repolarization. Prolongs APD and ERP. By prolong ERP, re-entry tachycardias can be abolished.
Adverse Effects
Thyroid Disturbances
Pulmonary Fibrosis
Pro-arrhythmias and Torsades de Pointes
Peripheral Neuropathy
Hepatitis
Cyanosis
Corneal Microdeposis
Indications
Ventricular and Supraventricular Arrhythmias
Ventricular Fibrillation (1st Line)
Recurrent Vtach
Class IV (CCB)
Digoxin Class V
Adenosine (Class V)
Agonist at cardiac A1 receptors in atrium, SAN and AVN resulting to reduce automaticity, conduction velocity and prolong refractory period. Negative dromotropic and chronotropic because it activates K+ channels.
Adverse Effects
Dysponea, Facial Flushing, Chest Pain
Class IA/IC
IA (Quinidine, Procainamide, Disopyramide)
IC (Flecainide, Propafenone)
Magnesium Sulfate (Class V)
Magnesium plays an important role in the transmembrane Ca2+ inflow and Ca2_ channel function. Mg2+ is nature's physiologic Ca blocker. An increase or decrease of Mg2+ within physiologic ranges inhibits or enhances intracellular calcium.
Indications
Torsades de Pointes
Treatment of Cardiac Arrhythmias caused by hypomagnesemia.
Adverse Effects
GI Discomfort
Hypermagnesemia
Ventricular
DC Cardioversion
Class I (Liodcaine)
IA (Quinidine, Procainamide, Disopyramide)
Also Reduces Phase 3
Quinidine - Cinchonism - Diarrhea, Rashes, Fever
IB (LignoCAINE, LidoCAINE)
Lidocaine - Tremmor, Confusion, Ataxia
IC (Flecainide)
Blocks fast sodium channels in non-nodal cells - Phase 0
Class III (Amiodarone)
Improve Cardiac Contractility
Inotropic Agents
Digoxin (Oral)
Indications
Chronic HF
Supraventricular Arrhythmias
Chronic Atrial Fibrillation
Increases intracellular Ca2+ by inhibiting Na+/K+ ATPase enzyme > Reduction in Ca2+ expulsion via Na/Ca exchange.
Adverse Effects
Heart Block
Supraventricular and Ventricular Arrhythmias
N/V, Diarrhea
Confusion, vertigo, hallucination, disorientation
Visual Disturbances
Gynecmastia
Beta Agonists (IV)
Indications
Acute HF in post MI
Cariogenic Shock
Increases Adenylate Cyclase, which helps in conversion of ATP to cAMP. This increases Ca2+ influx > Positive Inotropic Effect
DobutaMINE, DopaMINE, Isoprenaline
Adverse Effects
Arrhythmias
Increase myocardial oxygen demand
Bipyridines (IV)
Prevents breakdown of cAMP by reducing phosphodiesterase activity. This increases Ca2+ influx > Positive Inotropic Effect
Indications
Acute CF
Severe Exacerbation of Chronic HF
Adverse Effects
N/V
Arrhythmia
Thrombocytopenia
Liver Enzyme Changes
MilriNONE, InamriNONE
Reduce Preload
Diuretics (Oral)
Case 12
Diarrhea
Antimotility/Antisecretory
Opioids
Act on mu opioid receptors in myenteric plexus to inhibit Ach release and reduce motility. It reduces the frequency of abdominal cramps, decreases the passage of feces and shortens the duration of illness. Poor penetration of CNS therefore no alagesic or addictive properties.
Codeine
Loperamide
Diphenoxylate
Antimuscarinics
Atropine
Hyoscine
Dicycloverine
Propantheline
Racecadotril
Inhibits enkephalinase therefore prevent breakdown of opioids. Reduces the excessive intestinal secretion during episodes of diarrhea.
Adsorbents
Methylcellulose
Kaoilin
Charcoal
Absorb water and increase stool bulk. Adsorb intestinal microorganisms or toxins. Coat/protect the intestinal mucosa.
Agents that Modify Fluid Transport
Bismuth Subsalicylate
Stimulates the absorption of fluids and electrolytes by the intestinal wall and reduces stomach hypermotility.
Anti-infective agents
Cirpofloxacin
Cotrimoxazole
May be required in severe infection/bacterial gastroenterirtis.
Serotonin Receptor Antagonsits
Alosetron
Treatment of women who exhibit severe diarrhea-predominant IBS who have failed coventional therapy.
Constipation
Bulf Forming Laxatives
Ispaghula
Methylcellulose
Husk, bran
Increase stool bulk and absorb water forming a bulky hydrated mass. This increases intestinal distension, thereby increasing peristaltic activity. Colonic bacteria use the hydrated mass as a metabolic substrate > Increase bacterial cell mass while softening feces.
Osmotic Laxatives
Lactulose
Non absorbable compounds that hold water in the intestines by osmosis. By promoting an osmotic load, these agents trap increased volumes of fluid in the lumen. This distends the bowel increasing intestinal activity.
Fecal Softeners
Docusate Sodium
Liquid Paraffin
Surface-active agents similar to detergents. Agents become emulsified with the stool and soften/lubricate it for easy passage before diagnostic examination or surgery.
Stimulant Laxatives
Senna
Bisacodyl
Converted to their active forms by bacteria in the colon. They irritate the mucosa, iinducing low grade inflammation which stimulates peristalsis and promotes accumulation of water and electrolytes.
IBD
Aminosalicylates
MeSALAZINE
SulfaSALAZINE
Anti-inflammatory - Inhibit inflammatory mediators. Savenging free radicals and/or by decreasing neutrophil chemotaxis and superoxide generation.
Indications
UC
Corticosteroids
Severe UC and CD
TNF
AdalimuMAB
InflixiMAB
IBS
Antispasmodics
Hyoscine Butylbromide
Dicycloverine
Adverse Effects
Dry Mouth
Blurred Vision
Cardiac Arrhythmia
Case 4
Erythrocyte Factors
Vitamins
B9 (Folic Acid)
Leafy Green Vegetables
Folic Acid
Leucovorin (Folinic Acid)
Adverse Effects
Flushing
Pruritus
Rash
Indications
Megaloblastic and Macrocytic Anemia due to folate deficiency
Treatment and prevention of methotrexate toxicity
Prophylaxis for those at high risk
B12 (Cobalamin)
Cyanocobalamin (Oral/Parenteral), Hydroxocobalamin (Parenteral)
Indications
Pernicious Anemia
Vit B12 deficiency
Prophylactic after surgical operation that removes stomach and terminal ileum
Cyanide Poisoning
Adverse Effects
Flushing
Dizziness, Headache
Hypertension
Nausea and Diarrhea
Iron
Indications
IDA
Ferous Sulphate (Oral)
Adverse Effects
Constipation, N/V, Tarry stools
Acute toxicity
Chronic Toxicity
Death
Erythropoiesis-Stimulating Agents
EPOIETIN, DarbePOIETIN
Indications
Anemia
Prevention of Anemia
Adverse Effects
Fever, Arthralgia
Iron Deficiency
Increased blood viscosity - increase risk of thrombosis
Hypertension
Granulocyte Factors
FilGRASTIM, pegfilGRASTIM, LenoGRASTIM
Granulocyte Colony Stimulating Factor. Stimulates the production, maturation and activation of neutrophils.
Indications
Stimulation of granulocyte production in chemotherapy-induced neutropenia.
Promotes myeloid recovery in patient undergoing BMT.
Adverse Effects
Fever
Bone pain
Myalgia
Splenomegaly
Sargramostim
It is a recombinant granulocyte-macrophage colony-stimulating factor (GM-CSF)
Stimulates proliferation, differentiation and functional activity of neutrophils, eosinophils, monocytes and macrophages.
Indications
Reduce severity/duration of neutropenia induced by cytotoxic drugs following bone marrow transplant.
Promotes myeloid recovery after chemo
Treats drug induced bone marrow toxicity
Treats Neutropenia associated with AIDS
Treats Aplastic Anemia
Adverse Effects
Fever and Chills
Rash
Nausea
Bone Pain
Myalgia
Enlargement of liver and spleen
Platelet Factors
Oprelvekin
Recombinant interleukin-11, a thrombopoietic growth factor that directly stimulates the proliferation of hematopoietic stem cells and megakaryocyte progenitor cells and induces megakaryocyte maturation resulting in increased platelet production.
Indications
Prevents and Treats Chemotherapy-induced thrombocytopenia
Reduced the need for platelet transfusion following myelosuppressive chemotherapy.
Adverse Effects
Allergic Reactions
Tachycardia
Fever
Chills
Rash
Edema
Case 7
Bronchodilators
Beta 2 Receptor Agonists
SABA
Salbutamol, Levabuteroil
LABA
Salmeterol, Formoterol, Olodaterol
Stimulates B2 adrenergic Receptor - Bronchodilation
Adverse Effects
High cAMP causes cardiac and skeletal muscle contractions.
Mild Headache, muscle cramps
Savere: Tachycardia, hypokelemia, hyperglycemia, skeletal muscle tremors, anxiety, paradoxical bronchoconstriction
Muscarinic Antagonists
SAMA
Ipatropium
Adverse Effects
Tachycardia, Dry Mouth, Constipation, Nausea
LAMA
Triotropium
Tachycardia, Dry Mouth, Constipation, Nausea
Blocks M3 receptors. This reduces the background or stimulated parasympathetic activity. Bronchodilation
Xanthines (Theophylline) - Phosphodiesterase Inhibitor (Oral)
Inhibit the enzyme phosphodiesterase, that reduce cAMP to AMP. So there is more cAMP for dilation.
Adverse Effects
N/V, Headache, Stomach Pain, Diarrhea
Tachycardia, Arrhythmia< Dizziness, Seizure, Rash, Swelling, Difficult to Breath
Leukotriene Receptor Antagonists (LTRA) (Oral)
Blocks the receptor.
MonteLUKAST, ZafirLUKAST
Adverse Effects
Severe: Difficult in Breathing, Swelling, Rashes, Ear Pain
Mild: Heartburn, Diarrhea, Stomach Pain, Tiredness
Corticosteroids
Leukotriene Synthesis Inhibitor (Oral) - 5-Lipoygenase Inhibitors
Inhibit 5-Lipoxygenase in the Arachidonic Pathways. This results in less leukotrienes production. So decreased, bronchoconstriction, mucus secretions and decreased recruitment of immune cells which enhance airway inflammation.
Zileuton
Adverse Effects
Nausea, Diarrhea
Liver toxicity with jaundice, dark urine
Corticosteroids
Glucocorticoids (Cortisol)
Hydrocortisone
Cortisone
Dexamethasone
Prednisolone
Binds with glucocorticoid receptors. These receptors are found in almost every single cell. They have low affinity, so only activated in high levels.
Anti-inflammatory action.
Increase anti-inflammatory mediators (Increase annexin 1) which inhibit phospholipase A2.
Immuno-suppression - Decrease the production and activity of immune cells. Cortisol inhibits mediators of inflammation. Also acts on macrophages and reduce inflammatory cytokine release.
Promote body metabolism - gluconeogenesis, protein catabolism, lipolysis
Resistance to Stress - Provides energy if needed to combat stress
Indications
Anti-inflammation
Graft vs Host Disease - following blood or bone marrow transplantation.
Replacement therapy for patients with adrenocortical insufficiency.
Cancer treatment and palliative care.
Adverse Effects
Localized Infection
Thinning of skin
Delayed wound healing
Skin allergy, dermatitis, rashes, acne or hirsutism (abnormal hair growth in women)
Susceptibility to infection and poor recovery
Metabolism changes and fat deposition
Heart Disease and Hypertension
Muscle Wasting
Cataracts
Budesonide
Bethomethasone
Fluticasone
Minteralocorticoids (Aldosterone)
These receptors are only expressed in certain tissues (kidney, heart, colon, hippocampus). High affinity. Increase sodium reabsorption from the kidney, gut, sweat glands and salivary glands.
Fludrocortisone
Adverse Effects
Hypertension
Hypokelemia
Metabolic Acidosis
Hypersensitivity Reactions
H1 Antagonists (Antihistamines)
Block Action of Histamines in Capillaries. H1 is a Gq protein. Histamine binds to the active formation of H1 receptor and shifts the equilibrium further towards the active receptor state. This activates PLC. This causes the production of IP3 and DAG. This leads to calcium release causing smooth muscle contraction. Antihistamines are inverse agonists that shift the equilibirum towards the inactive state.
Cetirizine
Chlorphenamine (Cross BBB)
Adverse Effects
CNS Depression
Dry Mouth
Constipation
Case 11
Peptic Ulcer
Antimicrobial Agents
Clarithromycin
Amoxicillin
Metronidazole
Indications
Optimal Therapy for patients with H.pylori.
Eradication of H. pylori results in rapid healing of ulcer and low reoccurrence rate. To prevent recurrence = PPI + Amoxicillin + Clarithromycin/Metronidazole
PPIs (Oral)
Inactivate the H+/K+ ATPase in parietal cells. Neutral Omeprazole passes freely into the cytoplasm of parietal cells. It is a weak base. The acidic environment of the canaliculus converts omeprazole to its active sulfenamide form. Sulfenamide reacts with H+/K+ ATPase to form a covalent disulphide bond. Covalent binding inhibits the activity of the proton pump irreversibly.
OmePRAZOLE
Indications
Short term treatment for duodenal/gastric ulcer.
Gastric hypersecretory states - Zollinger-Ellison Syndrome
GORD
Prevention of NSAID induced ulcer.
H2 blockers (Oral)
CimeTIDINE
Ranitidine (Histamine)
Inhibits Histamine so inhibits Gs. So decreases adenylyl cyclase. Hence, stops H+/K+ pump.
Indications
Treatment for Dyspepsia
Heal Gastric and Duodenal Ulcers
Relieve GORD symptoms
Promote healing of NSAID-associated ulcers.
Cytoprotective Agents (Prostaglandins) (Oral)
Misoprostol
Stimulates prostaglandins. This stimulates Gi, which in turn inhibits adenylyl cyclase. Hence, stops H+/K+ pump.
Bismuth Salts
Has toxic effects to H. pylori and may also prevent its adherence to the mucosa or inhibit its bacterial proteolytic enzymes.
Indications
OTC remedy for mild GI symptoms
Combination regimens in eradication therapy.
Sucralfate
Complex of AlOH and sulfated sucrose, which releases aluminium in the present of acid. The residual complex carries a strong negative charge and binds to cationic groups in proteins. It can form complex gel with mucus, an action that is thought to decrease the degradation of mucus by pepsin and to limit the diffusion of H+ ions. Sucralfate can also inhibit the action of pepsin and stimulate secretion of mucus, bicarbonate and prostaglandins from the gastric mucosa.
Indications
Peptic Ulcer Disease
Indications
NSAID-induced peptic ulcer disease.
Contraindications
Pregnancy - increases uterine contractility.
Antacids
Weak Base that reacts with gastric acid to neutralize gastric acidity.
Systemic Antacids - Sodium Bicarbonate
Non-systemic Antacids - Al(OH)3, Mg(OH)2, CaCO3
Indications
Hyperacidity