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Term 2 (NSAID (Non-selective
Mostly reversible (Aspirin
Irreversible…
Term 2
Anaesthesia
Local: Sensation :red_cross:
General: Sensation, Consciousness :red_cross:
Sedation: Depression of awareness :fire:
General
Control of vitals :check:
Consciousness :red_cross:
Sensation :red_cross:
Muscle Relaxant :check:
- No evidence negative for pregnancy, but try not to, apendicitis. Otherwise analgesic
PKPD
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Inhaled
- MAC = ED50 (Minimum Alveolar Concentration) - Result in immobilization of 50% of patients
- Analgesics (LA / Opioids) decrease MAC
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Distribution:
- Lipid soluble = Inc potency
- Low solubility = Fast onset less drug dissolve in blood --> before Partial Pressure is high enough for it to diffuse out through BBB
Elimination
- Low solubility = Fast elimination
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Drugs
Inhaled
By MAC
Potency
Halothane (0.75%)
(+): Maintenance, Sweet Induction, children
(-): CVS, Respi, Liver
Isoflurane (1.4%)
(+): Maintenance
(-): CVS, Respi, Pungent
Enflurane (1.7%)
(+): Maintenance, less used
(-): Respi, CVS, Seizure, Renal
Sevoflurane (2%)
(+): Induction Sweet, Outpatients, rapid onset recovery
(-): Respi, CVS, Renal
Desflurane (6 - 7%)
(+): Outpatient, rapid onset recovery, Pungent
(Respi, CVS)
Nitrous Oxide (105%)
(+): Fast onset / Not soluble
(-): Post operative nausea, low potency
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Intravenous
Thiopental (Barbituate)
- Direct action on GABA
(+) Rapid onset, Distribution
(-) Direct acting, Respiratory Depression, Cerebral Depression
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Propofol
(+) Red post-op nausea & vomiting, Induction, Maintenance, Day surgery
(-) CVS depression
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Mechanism
- Affects Na+ K+ channels
- Direct activation of GABA channels (unlike BZ)
- Glycine receptors
- Glutamate receptors (NMDA, AMPA)
- Nicotinic receptors
Local
Control of Vitals :check:
Consciousness :check:
Sensation :red_cross:
Mechanism - Blocks Na+ channels of NERVE AXONS
- Unionized LA injected
- Enter Neuron easily (Unionized)
- Block intracellular h-gates of sodium gates
- Dec rate of depolarization
- Dec rate of repolarization
Use Dependent Block / Preferential Action
- High firing (Sensory) > Low firing (Motor)
- Circumferential > Deep
- Blocked/Active gates > Inactive gates
- Small neurons > Big neurons
- Myelinated > Non-myelinated
- Nociceptors > Sympathetic > Temp >Motor
Structure
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Neuron Structure
Structure:
- 4 domains (w segments)
- S4 voltage gated
- S6 dominant
- Between D3-4 h-gated
Factors:
- Lipid soluble, more potent, act longer
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PK
Absorption
- Dosage (Oral / IV)
- Binding to tissue REVERSIBLE
- High vascular tissue (Inc absorption PDC)
- Binds to albumin or a1 acid glycoprotein in blood
Metab/Excretion
- Water-soluble
- Urine
- Esters: By blood
- Amides: By liver
Factors affecting action:
- pH (Low pH more ionized, less action)
- Vasoconstrictors (prolong action)
- Hydrophobicity (prolong action)
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NSAID
Aspirin
Irreversible therefore
Strongest anti-platelet effect
Salicylic (Bind to Albumin)
Acetic acid free
PKPD
PK
- PK(A): Rapid absorb gut
- PK(M): Rapid metab acetic acid & salicylate @ tissue & blood
- PK(E): Excretion urine alkaline
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Inflammation
- Vascular permeability/dilation
- Cellular immune cells
- Pain mediators (Sensitize/Stimulate)
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General ADR
- Reduce prostaglandin
- Nausea, vomiting
- GIT ulcer
- Allergic
- Bleeding/Bruising
- Asthma
- Renal
PGE2: Inc Na+, Inc H2O
PGI2: Decrease aldosterone, Inc K+
COX2 - ADR
- Delayed follicular rupture
- Premature close of ductus arteriosus
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ACE inhibitor
ACE inhbitor
- Dec Ang II effects
- Dec vasoconstrict
- Dec aldosterone
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Adverse Effects
- Bradycardia/Asthma/Sedation
- Inc K/Angioedma/Dry cough/Teratanogenic/Renal fail
- Dec K/Na, Inc glucose/uria/lipid/Ca
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Mechanism:
- block b1 adrenergic receptor
- blocks Ang I to Ang II
- inhibit Na/Cl cotransporter
Pri: Idiopathic
Sec: Renal, Endo, Anat
Complications
- Congestive HF
- Stroke
- MI
- Renal Damage
- Stroke
Insulin Therapy
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Type 1: Insulin
Type 2: Lifestyle
Effects absorption
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Lispro/Aspart/Glulisine
Rapid
2-5hrs (P)
12-30mins
Clear
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Determir/Glargine
Long act (3/3)
24hrs (B)
1-4hrs
Clear, No mix
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Oral & Inject Hypoglycaemic Agents
Adv
Formin
1st Line Long term efficacy, safe No Hypoglycaemia; B/P 1st line T2 Duration 8-12h Urine
Litazone
Duration 24hrs Faecal, good for renal
Ide
clamide longest acting, 50-50 urine faece, rest mainly by urine; take before food
Linide
P short to 4hrs and rapid onset, glucose dependent reduce hypoglycaemia
Gliptin
Glucose dependent, Good for renal, Vilda- renal 100, Lina renal 5
Tide
Glucose dependent, Induce satiety Weight loss
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gliflozin
okay for hypoglycaemia, overweight, CVS
Drug
Insulin
Incretin - DPP4 inhibit
- glucose dependent secretagogue
- DPP4 breaks down GLP1, GIP
- Prolong endogenous incretin
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1st line Sensitizers: Biguanide
- Inc insulin receptor
- Dec glucose release liver
- Dec intestinal glucose absorption
- Dec glucagon
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Disadv
Formin
1st Line Long term efficacy, safeNo Hypoglycaemia; B/P 1st line T2 Duration 8-12h Urine
Litazone
Bone fracture, Weight gain, Edema, Heart failure-Rosi, induce CYP450 Imagine a Fat man
Ide
Weight gain, hypoglycemia esp hepatic impairment, allergy
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Gliptin
Expensive, GIT nausea, diarrhoea, stomach pain, Flu, headache, skin, caution pancreatitis
Tide
Expensive, GIT, nausea, vomiting, diarrhea, history of pancreatitis
Acarbose
Flatulence; Contra: GIT, IBS, Renal, Hepatic, not preferred lower efficacy tolerance
gliflozin
UTI, inc urination, female genital mycotic yeast infection, diabetic ketoacidosis and lower limb amputation
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Anti-epileptic
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Drugs
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Phenytoin
- Inc brain GABA
- Dec excitability Na, Ca
- Inc hyperpolarization (more -ve)
- Swelling / Bleeding gums
Carbamazepine
- Inc brain GABA
- Dec excitability Na, Ca
- Inc hyperpolarization (more -ve)
- Also used for Chronic orofacial pain / mood disorders
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Adverse
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Teratogenic
- Phenytoin
- Carbamazepine
- Phenolbarbitone
- Valproate
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Efficacy
Hypo risk glucose dependent/low risk of hypo
Weight loss / gain
Side effects (Cardiac, Renal, Hepatic)
Flatulence
Cost
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