Drugs - Pharmacology, Metabolism, Special Notes and Pharmacokinetics Flashcards

(124 cards)

1
Q

1 - 3 Mild Pain Analgesic Requirements

A

May not require analgesia
Consider non pharmacological approaches
Consider non opiod analgesia - paracetamol, ibuprofen

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2
Q

4 - 6 Moderate Pain Analgesic Requirements

A

Consider:
mild pain analgesic steps
non opioid analgesia - Paracetamol, ibuprofen

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3
Q

7 - 10 Severe Pain Analgesic Requirements

A

Consider mild and moderate treatment steps

Will require NAS, IM, IV analgesia - Penthrane, fentanyl, morphine

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4
Q

Adrenaline Metabolism

A

Metabolised by sympathetic nerve endings and subject to mitochondrial enzymatic breakdown by monoamine oxidase at the synaptic level

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5
Q

Adrenaline pharmacology in asthma

A

sympathomimetic agent that is an alpha and beta adrenergic receptor antagonist that makes the heart beat faster and harder due to alpha 1 causing peripheral vasoconstriction and beta 1 increasing ventricular irritability, contractile force, conductivity and AV node. Beta 2 stabilises mast cells to negate their deregulatory effect

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6
Q

Adrenaline pharmacology in anaphylaxis

A

sympathomimetic agent which is an alpha and beta adrenergic receptor antagonist that makes the heart beat faster and harder due to alpha 1 causing peripheral vasoconstriction and beta 1 increasing ventricular irritability, contractile force, conductivity and AV node. Beta 2 stabilises mast cells to negate their deregulatory effect

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7
Q

Adrenaline pharmacology in cardiac arrest

A

sympathomimetic agent which is an alpha and beta adrenergic receptor antagonist that makes the heart beat faster and harder due to alpha 1 causing peripheral vasoconstriction and beta 1 increasing ventricular irritability, contractile force, conductivity and AV node. Beta 2 stabilises mast cells to negate their deregulatory effect

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8
Q

Adrenaline pharmacology in croup

A

reduces bronchial and tracheal epithelial permeability decreasing airway oedema, increasing airway radius and improving airflow.

It improves Westley Croup Scores at 30 minutes.

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9
Q

Adrenaline Special Notes

A

1: 1,000 (1 mg/mL) adrenaline (epinephrine) presentation should be used for all nebuliser administration
1: 10,000 (100 microg/1 mL ) or a 1 : 100,000 (10 microg/1 mL ) adrenaline (epinephrine) preparation should be used for all low dose IM/IV injections

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10
Q

Aspirin Metabolism

A

converted to salicyclic acid primarily in the GI mucosea and liver
excreted by the kidneys

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11
Q

Aspirin Pharmacology

A

prevents platelets from aggregating to exposed collagen fibres at the site of vascular injury

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12
Q

Aspirin Special Notes

A

Patients with suspected ACS or acute pulmonary oedema who have had less than 300 mg aspirin in the previous 24 hours should be administered a dose of aspirin that equates to a total daily dose of 300–450 mg

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13
Q

Ceftriaxone Metabolism

A

Excreted as a variety of active and inactive metabolites through urine, bile and faeces

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14
Q

Ceftriaxone Pharmacology

A

A third generation cephalosporin antibiotic with a bactericidal action

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15
Q

Ceftriaxone Special Notes

A

Due to adverse affects associate with IM administration, IV administration is preferred

Rapid administration of large doses may result in seizures due to high sodium content

All cannula and IV lines must be flushed thoroughly with sodium chloride 0.9% following each administration

Prepared in aseptic manner

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16
Q

Dexamethasone Metabolism

A

metabolised by the liver and excreted by the kidneys

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17
Q

Dexamethasone Pharmacology

A

Long-acting synthetic corticosteroid that produces anti-inflammatory and immunosuppressive effects

Presumed effect is vasoconstrictive actions in the upper airway, followed by systemic antiinflammatory effect

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18
Q

Dexamethasone Special Notes

A

the preferred corticosteroid for the treatment of croup due to its lower hospital re-presentation rate

All patients administered dexamethasone for the treatment of croup must be transported to an appropriate health facility for assessment

The Westley Croup Score must be used by all officers to assess croup severity

Administer with syringe or clean spoon

Mix with small amount of sweet ingestible liquid

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19
Q

Fentanyl Metabolism

A

metabolised by the liver, excreted by the kidneys

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20
Q

Fentanyl Pharmacology

A

synthetic narcotic analgesic that acts on the central nervous system by binding with the opioid receptors

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21
Q

Fentanyl Special Notes

A

When combined narcotic (morphine and fentanyl) therapy is administered, the total max dose must be calculated using a combination of all morphine and MME (eg fentanyl) medication

Hypotensive adult Pts (SBP 90 mmHg) all incremental fentanyl doses must be no greater than 25 microg for IV and 50 microg for IM

CCP backup required in fentanyl administration to hypotensive pts

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22
Q

Glucagon Metabolism

A

Metabolised by the liver, kidneys and in the plasma

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23
Q

Glucagon Pharmacology

A

Hyperglycaemic agent that mobilises hepatic glycogen which is released into the blood as glucose with inotropic and chronotropic effects not mediated through beta-receptors

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24
Q

Glucagon Special Notes

A

Oral carbs should be given when the Pt has responded to glucagon to restore liver glycogen and prevent secondary hypoglycaemia

low threshold for glucagon administration in hypotensive/shocked anaphylaxis Pts when presenting with heart failure and/or prescribed beta blocker therapy

Prepare in aseptic manner, disinfect rubber stopper of vial with antimicrobial swab and allow to dry before piercing

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25
Glucose 10% Metabolism
Broken down in most tissues and distributed throughout total body water
26
Glucose 10% Pharmacology
A sugar that is the principal energy source for body cells, especially the brain
27
Glucose 10% Special Notes
the preferred treatment for hypoglycaemia for patients unable to take oral glucose due to its rapid onset and ability to quickly restore blood glucose concentration to normal values
28
Glucose Gel Metabolism
Broken down in most tissues and distributed throughout total body water
29
Glucose Gel Pharmacology
Quickly absorbed in the intestinal tract - principal energy source for body cells, especially the brain.
30
Glyceryl trinitrate (GTN) Metabolism
readily absorbed and metabolised by the liver
31
Glyceryl trinitrate (GTN) Pharmacology
decreases preload and afterload, dilates blood vessels to allow blood through the coronary veins and arteries and pools blood in peripheral veins
32
Glyceryl Trinitrate (GTN) Special Notes
Subling GTN first line Tx for ACS, however IV GTN should be considered as part of the mgmt regime for all Pts unresponsive to subling GTN, narcotics and/or blockers GTN is first line Tx for autonomic dysreflexia, however morphine should be considered as part of the mgmt regime if Pt unresponsive to initial Tx
33
Hydrocortisone Metabolism
Metabolised by the liver, excreted by the kidneys
34
Hydrocortisone Pharmacology
Inhibit the inflammatory action of the phospholipase A2 enzyme and used for multiple reasons for infections in a variety of setting for long term disease processes
35
Hydrocortisone Special Notes
Each 100 mg hydrocortisone vial is to be reconstituted with 2 mL sodium chloride 0.9% or water for injection All canulae and IV lines must be flushed thoroughly with sodium chloride 0.9% following each medication administration Prepare in aseptic manner, disinfect rubber stopper with antimicrobial swab and allow to dry before piercing
36
Ibuprofen metabolism
Metabolised by the liver and exreted mainly by the kidneys
37
Ibuprofen pharmacology
Non-selective NSAID that inhibits the synthesis of prostaglandins resulting in analgesic, antipyretic and anti-inflammatory actions
38
Ibuprofen Special Notes
Consider previous doses by the Pt, carer, parent or guardian Administer with or shortly following food/milk Can be used in conjunction with paracetamol for additional pain relief
39
Ipratropium bromide Metabolism
metabolised by the liver and excreted by the kidneys
40
Ipratropium bromide Pharmacology
Antimuscurinic agent that promotes bronchodilation by inhibiting cholinergic bronchomotor tone
41
Ipratropium bromide Special Notes
Must be administered in conjunction with salbutamol - solutions may be mixed and administered via the same nebuliser mask
42
Loratadine Metabolism
absorbed in the GI tract with rapid first-pass hepatic metabolism
43
Loratadine Pharmacology
long acting, second generation peripheral histamine H1 receptor antagonist
44
Loratadine Special Notes
Antihistamines have no role in the Tx or prevention of respiratory or cardiovascular symptoms in anaphylaxis May be administered with or without food
45
Methoxyflurane metabolism
Metabolised by the liver and excreted mainly by the lungs
46
Methoxyflurane pharmacology
More susceptible to metabolism than other halogenated ethers and has a greater propensity to diffuse into fatty tissue
47
Methoxyflurane Special Notes
At no time should unconsciousness be deliberately induced using methoxyflurane The lowest dose of methoxyflurane to provide analgesia should be used Pt not to be left unattended If the Pt prefers simultaneous inhalation through both nose and mouth, the inhaler may be connected into a standard anaesthetic face mask prior to administration Only one dose of 3 mL should be administered per Pt whilst in the ambulance No single officer should administer more than 2 doses in the ambulance per shift Where possible, ambulance should be adequately ventilated
48
Midazolam Metabolism
Metabolised by the liver, excreted by the kidneys
49
Midazolam Pharmacology
Short acting CNS depressant that enhances the action of the inhibitory neurotransmitter GABA, inducing amnesia, anaesthesia, hypnosis and sedation
50
Midazolam Special Notes
Focal seizure activity in an unconscious or altered (GCS_\<_12) treated as a generalised seizure - GCS \>12 contact QAS Clinical Consultation and Advice Line Take into account previous doses prior to arrival of midazolam or diazepam Contact QAS Clinical Consltation and Advice Line if not responding to QAS initiated Tx First dose of midazolam for seizures must be administered NAS or IM injection unless IV cannula already in situ All IV doses must be diluted with sodium chloride 0.9% to make 5 mg midazolam in 5 mL presentation
51
Morphine Metabolism
Metablised by the liver, kidneys and lungs
52
Morphine Pharmacology
Narcotic analgesic that acts on CNS by binding with opioid receptors altering pain perception processes and emotional response to pain. Causes respiratory depression, vasodilation, decreases gag reflex and slows AV node conduction.
53
Morphine Special Notes
When combined narcotic (orphine and fentanyl) therapy is administered, the total maximum dose is to be calculated using a combination of all morphine and morphine milligram equivalent (MME) medication (eg fentanyl), eg 10 mg morphine and 100 microg fentanyl would equl the ACP total max dose of 20 mg MME When administered to hypotensive Pt, ACPs must call for CCP backup where available Hypotensive adult Pts (SBP \< 90 mmHg), all incremental morphine doses are to be no greater than 2.5 mg IV or 5 mg IM Single IM dose morphine is suitable anagesic for moderate to severe labour pain in full term mothers. Advise receiving hospital of dose.
54
Ondansetron Special Notes
ampoules should be protected from light IV cannula not to be inserted for ondansetron administration only transient adverse effects have been reported with rapid IV injections
55
Ondonsetron Metabolism
metabolised by the liver and excreted by the kidneys
56
Ondonsetron Pharmacology
Serotonin 5-HT3 antagonist which inhibits the vagus nerve and blocks serotonin receptors in the chemoreceptor trigger zone
57
Oxygen Metabolism
N/A
58
Oxygen Pharmacology
A colourless, odourless gas essential for the production of cellular energy
59
Oxygen Special Notes
Diving accidents are not covered by this DTP - administer high flow oxygen Sat monitors unable to differentiate between carboxyhaemoglobin and oxyhaemoglobin, therefore carbon monoxide poising Pts must be administered the maximum oxygen dose irrespective of SpO2 readings COPD Pts must have a rate of 6 L/min - all other Pts at 8 L/min FiO2 levels influenced by delivery systems, rep rate and open or closed mouth
60
Oxytocin Metabolism
metabolised by the liver and excreted by the kidneys
61
Oxytocin Pharmacology
Stimulates uterine contractions by altering calcium concentrations within the uterine muscle cells increasing it tonicity
62
Oxytocin Special Notes
Oxytocin is only to be administered to the consenting patient - women who prefer a physiological management must birth the placenta unaided, by maternal effort and the natural force of gravity to allow for the benefits of delayed cord clamping it is acceptable to do a modified active third stage management by waiting until the cord has stopped pulsating to administer oxytocin. This is particularly important in neonatal resuscitation where the baby is resuscitated between the mum's legs to receive the benefit of a pulsing cord and placental perfusion.
63
Paracetamol Metabolism
Metabolised by the liver, excreted by the kidneys
64
Paracetamol pharmacology
A p-aminophenol derivative that exhibits analgesic and antipyretic activity. It does not possess significant anti-inflammatory activity
65
Paracetamol Special Notes
Consider previous doses administered May be administered with or without food
66
Salbutamol Metabolism
metabolised by the liver, excreted by the kidneys
67
Salbutamol Pharmacology
Acts on B2 adrenoreceptors causing bronchodilation, inotropic and chronotropic actions. It stimulates the sodium/potassium ATPase pump, increasing intracellular K+ and reducing serum K+. ``` inotropic = heart contractility chronotropic = increased HR ```
68
Salbutamol Special Notes
When clinically appropriate, MDI is preferred to minisise aerosol generation, especially if infectious Different preparation for IM and IV - using the incorrect one will cause serious adverse effects COPD Pts received NEB salbutamol at 6 L/min, all other Pts at 8 L/min Nebulised salbutamol will reduce serum potassium by 0.5 - 1 mmol/L within 30 minutes Nebules to be stored within foil packet and discarded three months after opening - write date on packet when opened
69
Sodium chloride 0.9% metabolism
100% bioavailability. Excess sodium is predominantly excreted by the kidneys.
70
Sodium chloride 0.9% pharmacology
Electrolyte replenisher for maintenance or replacement of fluid and a vehicle for parenteral drug administration
71
Sodium Chloride 0.9% Special Notes
Use of volume expansion in uncontrolled haemorrhage (without concurrent TBI) may be associated with poor outcomes - only administer the minimum amount of IV/IO fluid to maintain a radial pulse Hypotension with a concurrent TBI is associated with poor outcomes - only administer the minimum amount of IV fluid required to maintain a systolic BP 100 - 120mmHg (adult) Excessive fluid infusion may lead to neurogenic pulmonary oedema in the spinal cord injured patient Too rapid infusion of fluids in a patient without fluid deficit, or with underlying cardiac problems, may cause pulmonary oedema and congestive heart failure A gentle fluid challenge may be considered for patients with suspected right ventricular infarct (following 12-Lead ECG acquisition with V4R) and no signs of left ventricular failure (e.g. pulmonary oedema) BD PosiFlushSP pre-filled are for vascular devices only and NOT for any dry product reconstitution AND/OR medication dilution
72
Sucrose 24% Metabolism
mucosal absorption with hepatic metabolism
73
Sucrose 24% Pharmacology
increases endogenous opioids resulting in approximately 5−8 mins of analgesia in infants
74
Sucrose 24% Special Notes
Alternate support measures (e.g. breast feeding, appropriate positioning, distraction) should always precede oral sucrose administration Oral sucrose is not considered appropriate for the management of continuing pain or distress Oral sucrose to manage mpain should be used in conjunction with analgesics (eg paracetamol, NAS fentanyl)
75
Tranexamic Acid (TXA) Metabolism
metabolised by the liver, excreted by the kidneys
76
Tranexamic Acid (TXA) Pharmacology
Stops the conversion of plasminogen to plasmin, stopping the breakdown of fibrin and promoting clot strength, inhibiting lysis.
77
Water for injection metabolism
N/A
78
Water for injection pharmacology
Sterilised H2O
79
Water for Injection Special Notes
QAS medications approved for dilution with water for injection include: ceftriaxone, glucagon, hydrocortisone and ketamine Water for injection may be used to assist with the administration of oral medication if required (aspirin, clopidogrel, paracetamol and ticagrelor)
80
Amiodarone Pharmacology
blocks Na+, K+, Ca++, alpha & beta channels prolonging action potential & refractory period, decreases excitability & improves potential for ROSC
81
Amiodarone Metabolism
Majority is excreted by the liver and GI tract in biliary excretion, may be some hepatic recirculation
82
Amiodarone Special Notes
* If the Pt is on oral amiodarone cardic arrest administration is authorised * Pts with Torsade de Pointes due to suspected prolonged QT interval from excess amiodarone magnesium sulphate should be considered - contct QAS Clinical Consultation and Advice Line
83
What are the four main concepts of pharmacokinetics?
Absorption Distribution Metabolism Excretion
84
What is drug absorption?
Route of administration
85
What is drug distribution?
Lipid solubility Perfusion & transportation
86
What is drug metabolism?
Hepatic first-pass effect Biotransformation
87
What is drug excretion?
Elimination & excretion
88
Factors affecting drug distribution
Lipid solubility Plasma protein binding Body composition Tissue and organ perfusion Organ function
89
How does lipid solubility affect drug distribution?
influences in which body compartments the drug may accumulate, directly affecting drug effect and dosage schedules
90
How does plasma protein binding affect drug distribution?
affects bioavailability and transportation of the drug
91
How does body composition affect drug distribution?
relative proportions and absolute amount of lean and adipose tissues
92
How does tissue and organ perfusion affect drug distribution?
impacts distribution of the drug throughout the body, and therefore effect, metabolism, and excretion
93
How does organ function affect drug distribution?
relates to those organ systems involved in the metabolism, elimination, and excretion of the drug
94
What is the primary drug distribution issue or paramedics?
tissue perfusion, and therefore cardiac function, blood pressure, and shock
95
What is the secondary drug distribution issue for paramedics?
functionality of kidneys and liver, for metabolism and excretion
96
Atropine Pharmacology
* 1. Anticholinergic action inhibits vagus innervation of the heart * 1. loss of parasympatheic tone resulting in increased heart rate and contractility
97
Sodium bicarbonate Pharmacology
Provides extracellular sodium to overcome Na+ blockade Reverses metabolic acidosis by reacting with H+ ions
98
Calcium gluconate Pharmacology
* Improves contractility * Myocardial protection in hyperkalaemia * Provides extracellular calcium to overcome Ca++ blockade
99
Magnesium sulphate Pharmacology
Stabilises the membrane in Torsades de Points by reducing Ca++ influx into the cell
100
Naloxone Pharmacology
opioid antagonist that prevents or reverses the effects of opioids including respiratory depression, sedation and hypotension. Naloxone antagonises the opioid effects by competing for the same receptor sites.
101
Naloxone Metabolism
hepatic
102
Naloxone Special Notes
* should only be administered following adequate patient oxygenation and ventilation * should be administered cautiously to patients who are known or suspected to be physically dependent on narcotics * not required in the vast majority of cases, and the patient will need only supportive therapy followed by transport * duration of the narcotic may exceed that of naloxone and renarcotisation is possible * Administration in the pre-hospital environment may unmask potentially unwanted side effects in the setting of poly pharmacy overdose * should not be administered to the newly born, even in the setting of suspected or identified opiate exposure/overdose, as administration of naloxone may lead to acute withdrawal and seizures
103
Droperidol Pharmacology
Dopamine-2 receptor antagonist that increases brain turnover of dopamine; and Mild alpha-adrenergic receptor blockade which can result in mild hypotension
104
Droperidol Metabolism
Hepatic metabolism with biliary/renal excretion as inactive metabolites
105
Droperidol Special Notes
Where a second dose of droperidol has been administered by an ACP2, a CCP must be requested and they may be cancelled if the second dose of droperidol achieves the desired sedation effect Dosages and times of administration prior to QAS arrival must be considerd to ensure compliance with the QAS Droperidol DTP In Lewy body dementia, antipsychotic (e.g. droperidol) can cause deterioration in cognitive and motor function, and may paradoxically increase agitation and worsen behaviour For other presentations of dementia (e.g. Alzeheimer’s disease) droperidol is a suitable pharmacological agent for the management of acute behavioural disturbance Under no circumstances is an IV cannula to be inserted for the sole purpose of droperidol administration. IV droperidol administration is only to occur when an IV cannula is already insitu
106
Magnesium Sulphate Pharmacology
It causes vasodilation and bronchodilation through inhibition of smooth muscle contraction. Magnesium ions also possess anticonvulsant and anti-dysrrhythmic properties
107
Magnesium Sulphate Metabolism
filtered in the kidneys and excreted predominantly in urine with small amounts in faeces and saliva
108
Box Jellyfish Antivenom Pharmacology
contains concentrated immunoglobulin that acts to neutralise the toxins present in the venom of the box jellyfish
109
Box Jellyfish Antivenom Metabolism
Hepatic and in muscle tissue
110
Box Jellyfish Antivenom Special Notes
* The dose of antivenom is related to the dose of venom, not based on the size of the patient * At all times during antivenom therapy adrenaline (epinephrine) * must be available in case of an anaphylactic reaction. If reaction * occurs, immediately cease the administration of box jellyfish * antivenom and treat patient in accordance with CPG: Anaphylaxis * and allergy. * IV injection is the preferred route of administration for all indications. * If a patient is in cardiac arrest due to box jellyfish envenomation, the box jellyfish antivenom is only to be administered following the commencement of effective CPR, advanced life support measures and administration of cardioactive drugs * Box jellyfish antivenom must be protected from light and stored between 2–8°C. DO NOT FREEZE
111
Hydroxocobalamin Pharmacology
(an injectable form of vitamin B12), binds with circulating and cellular cyanide to form cyanocobalamin, which is then excreted in urine
112
Hydroxocobalamin Metabolism
excreted by the kidneys
113
Hydroxocobalamin Special Notes
* Hydroxocobalamin infusions are only to be administered by appropriately trained QAS clinicians within the following response catchments: - Central Queensland District: Orica Yarwun Cyanide Plant - Darling Downs District: Texas Silver Mine - North West District: Great Australian Mine, Lorena Gold Project * Substantial increases in blood pressure may occur * There are no adequate and well-controlled studies of hydroxocobalamin * administration in pregnant women. Hydroxocobalamin should be used * during pregnancy ONLY if the potential benefits justifies the potential * risk to the fetus
114
Ketamine Pharmacology
a rapid acting dissociative anaesthetic agent that is primarily an NMDA receptor antagonist but also interacts with opioid, monoaminergic, muscarinic receptors and voltage sensitive Ca ion channels
115
Box Jellyfish Antivenom Pharmacology
contains concentrated immunoglobulin that acts to neutralise the box jellyfish toxins
116
Clopidogrel pharmacology
selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet receptor, thereby inhibiting platelet aggregation
117
Clopidogrel metabolism
Hepatic metabolism with near equal amounts excreted in urine and faeces
118
Clopidogrel special notes
15–48% of patients have a poor platelet inhibition response to clopidogrel. Therefore, the interventional cardiologist may request the administration of ticagrelor
119
Enoxaparin pharmacology
Binds to antithrombin III and inhibits thrombin generation and factor Xa and thrombin
120
Enoxaparin metabolism
Hepatic but mostly eliminated unchanged
121
Enoxaparin special notes
IV administrations an enoxaparin 60 mg/0.6 mL graduated pre-filled syringe must be used. The air bubble MUST NOT be administered with the medication. SUBCUT administrations an enoxaparin 100 mg/1 mL graduated pre-filled syringe must be used. The volume to be injected (1 mg/kg) should be measured precisely using the markings on the syringe. When adjusting to the correct dose, hold the syringe with the needle tip pointing down. Depress the plunger so the bottom of the air bubble is level with the marking on the syringe that corresponds to the dose required. The air bubble is required to be administered with the medication.
122
What is the pharmacology of Sodium Bicarbonate?
hypertonic solution that reacts with excess hydrogen ions forming carbon dixoide and water, restoring plasma pH levels
123
What is the metabolism of Sodium Bicarbonate?
to C02 and H2)
124
What is the pharmacology of droperidol?
Antagonises dopamine receptors in the CNS