For further information on drugs, please call:

Drug Information Service (DIS)

Pharmacy Department ,

Hospital Jasin (Ext 501/507)

online1.mimsgateaway.com.my

username & password: please refer to pharmacy

Open for all

healthcare provid-

VOLUME 2/2015

Ramadhan Al-Mubarak:

Medicines Use

Vancomycin :

Pharmacokinetics &

Pharmacodynamic

High Alert Medication

Hospital Jasin

PEDIATRIC SYRUP

DOSING

16-17

2

CO

NT

EN

TS

3-4

5-6

7-10

Vancomycin:Pharmacokinetics & Pharmacodynamics

Ramadhan Al-Mubarak: Medicines Use

11-13 Drug Comparison

Heparin, Fondaparinux, Enoxaparin

14-15

Pediatric Syrup Dosing 16-17

18

Diabetic Medication Adherence Therapy Clin-ic

22-23 Pharmacy Activities

High Alert Medication

Advisor

Nursahjohana Md Sahak

Noorazlinda Yacob

Izrul Azwa Mohd Latiff

Editors

Contributors

Ng Shy Png Low Jia Hui

Nur Athirah Haziqah Mohamad Sobri Mo-

Top 20 purchased drug 2014

Tan Xin Yi

PEDIATRIC SYRUP

DOSING

Dr Zaleha Bt Md Noor

ADR Report 2014 19 Medication Error

20-21

7-10

23

Date Title

2.4.2015 Taklimat Medication Error

24.4.2015 Taklimat Pencegahan Kebakaran

14.5.2015 MIMS Gateway User Training

15.5.2015 Laserband-Wristband

27.5.2015 Kenali Ubat Anda & Pelaksanaan 5S

29.5.2015 Know Your Medicines

11.6.2015 Taklimat Kesedaran EKSA

13.6.2015 Use of Galvusmet in the latest treatment of Type-2 DM

CME Organized By Pharmacy Department

10 LANGKAH KENALI UBAT ANDA

30.5.2015 Taman Botanikal Melaka

22

Vancomycin is an antibiotics to treat patients infected with methicillin-

resistant Staphylococcus aureus and methicillin-resistant coagulase-

negative Staphylococcus species.

Pharmacokinetic & Pharmacodynamic By :Nursahjohana bt Md Sahak

Pharmacokinetic profile

Not absorbed orally

ABSORPTION

penetrates into most body spaces & dependent on the degree of inflam-mation present

α-distribution phase of 30 min to 1 hour

β-elimination half-life of 6–12 hour volume of distribution is 0.4–1 L/kg. Protein binding ~50%

There is no apparent metabolism

EXCRETION

eliminated primarily via the renal route

Pharmacodynamic profile

Vancomycin is a concentration-

independent antibiotic (also referred to as a “time-dependent” antibiotic), and there are factors that affect its clinical activity, such as tissue distribution, inoculum size, and emerging resistance.

Common toxicity Ototoxicity (<2%) Nephrotoxicity (increased risk at trough

concentrations greater than 15 mcg/ml) -Risk factors include: Obesity

High dose/trough

Long duration

Concomitant nephrotoxins

ICU stay

Vasopressors 3

METABOLISM

DISTRIBUTION

No Parameters Remarks

1 Vancomycin trough level

Obtain at steady-state;

For normal renal function: After the 3rd dose

For renal impairment: After the 1st dose

Therapeutic serum concentration: For serious infections, such as bacteremia, infective endocarditis, osteomyelitis, meningitis, pneumonia, and severe SSTI (eg, necrotizing fasciitis) due to MRSA, vancomycin trough concentrations of 15 to 20 mcg/ml are recommended. For less serious infections such as skin and soft tissue infections, trough concentrations of 10 to 15 mcg/ml are recommended.

2 BUN & serum creatinine

Measure every 2 days or every day in unstable renal function

3 Body weight Measure every 2-7 days

4 Urine output Measure and monitor urine output daily

5 Baseline audi-ograms

Measure baseline and weekly audiograms (If applicable)

6 Phlebitis Check for signs of phlebitis daily

A histamine-mediated reaction, often called 'red man syndrome', involves a rash over the upper body, possibly accompanied by hypotension. The syndrome is thought to be related to peak serum concentration.

Red man syndrome has often been associated with rapid infusion of the first dose of the drug 4

Prescribing

error

(26)

59%

Dispensing

error(18)

41%

Process in which errors occured

Total ME's reported = 44 cases

Doctor

(26)59%

Pharmacist

asisstant(17)

39%

Provisional

Registered

Pharmacist

(PRP)

(1)

2%

Categories made initial error

References : (1) Guideline on Medication Error Reporting, 1st edition July 2009

(2) Minit Mesyuarat Jawatankuasa Ubat & Terapeutik Hospital Jasin, Bil 1/2015

MEDICATION ERROR (ME) REPORT IN HOSPITAL JASIN 2014

21

Medication Error (ME) Report Form All medication errors involving any medicine should be reported. Medication error data collected will be used in formulating strategies to further improve the quality and safety of medication use. (Source: Guideline on Medication Error Reporting, Ministry of Health, 2009)

MEDICATION ERROR

Medication Error (ME) is any preventable event that may cause or lead to inappropriate medication use or patient harm while the medication is in the control of the health care professional, patient or consumer.

Such event may be related to professional practice, health care products, procedures and systems, including

- prescribing

- order communication

- product labeling

- packaging and nomenclature

- compounding

- dispensing

- distribution

- administration

- education

- monitoring

- use

TYPES OF MEDICATION ERROR (ME)

(1) Prescribing error

(2) Omission error

(3) Wrong time error

(4) Unauthorised drug error

(5) Dose error

(6) Dosage form error

(7) Drug preparation error

(8) Route of administration error

(9) Administration technique error

(10) Deteriorated drug error

(11) Monitoring error

(12) Compliance error

(13) Other medication error

20

B Y : N U R A T H I R A H H A Z I Q A H B I N T I M O H A M A D S O B R I

Ram

adhan A

l-M

ubara

k: M

edic

ines u

se

NO

OR

AZ

LIN

DA

Y

AC

OB

Administration routes DO NOT nullify fasting:

5

Eye drops

Ear drops

Nitroglycerin tablets placed under the tongue for the treatment of angina

All substances absorbed into the body through the skin, such as creams, ointments, and medicated plasters

Nasal spray

Injections through the skin, muscle, joints, or veins, with the exception of intravenous feeding

Mouthwash, gargle, or oral spray, provided nothing is

swallowed into the stomach.

Administration routes DO nullify fasting:

Inhaler Pessaries, suppository, enema, vaginal washes or any medical ovules, that inserted to vagina or anus

Surgery involving general anaesthesia

How to adjust administration time of

medicine?

6

References

Panduan Berpuasa Bagi Pesakit Terbitan JAKIM 2013

Risalah Puasa Dan Ubat, Bahagian Perkhidmatan Farmasi

INSTRUCTION HOW TO TAKE

ONCE DAILY before/after food

Choose the appropriate time suitable to you and follow that timing throughout the

fasting month. For medicine to be taken before food, take

the medicine with water. Take your food between 30 and 60 minutes later.

TWICE A DAY AFTER FOOD

Take after iftar and during sahur

3 TIMES A DAY AFTER FOOD

After iftar Before sleep (Take small quantity of food) During sahur

TWICE A DAY BEFORE FOOD

Take the medicine after breaking fast with water. You can start eating between 30 and 60 minutes later.

3 TIMES A DAY BEFORE FOOD

Follow the above instruction, and take once more before bedtime.

TOP 5 MOST COMMONLY

REPORTED ADVERSE DRUG

REACTION (ADR) IN 2014

NO ADR REPORTED

NO. OF CASES

1 Headache 10

2 Vomiting 8

3 Dizziness 7

4 Itchiness 4

5 Diarrhea 3

Total ADR’s reported are 39 cases.

Most commonly medicines that caused ADR in 2014 are antibiotics,

cardiovascular drugs and analgesics.

19

Report On Suspected Adverse Drug Reactions (ADR)

Report on Suspected Adverse Drug Reactions (ADR) is a tool for the Ministry of Health to monitor new safety concerns that might be related to a marketed product. Based on an evaluation, Ministry of Health may take regulatory action to improve product safety such as restrictions in use, refinement of dosage instructions and strengthening of specific warning. ADR can be reported online through http://portal.bpfk.gov.my and a copy should be sent to Pharmacy Department/Unit. (Source: Malaysian Guideline For The Reporting and Monitoring Of Adverse Drug Reaction, Ministry Of Health, 2002)

B Y : N U R A T H I R A H H A Z I Q A H B I N T I M O H A M A D

S O B R I

B Y : N U R A T H I R A H H A Z I Q A H B I N T I M O H A M A D S O B R I

NO MEDICINES PURCHASED VALUE (RM)

1 Sodium Chloride 0.9% in 500ml Inj 70,083.30

2 Streptokinase 1,500,000 units Inj 54,879.60

3 Finasteride 5mg Tab 46,475.00

4 Heparin Sodium 5000 IU/ml in 5ml Inj 41,099.96

5 Metformin HCl 500mg Tab 38,646.43

6 Amoxycillin & Clavulanic Acid 625mg Tab 36,875.34

7 Cloxacillin Sodium 250mg Cap 36,372.96

8 Lanthanum Carbonate 1000mg Tab 32,397.87

9 Haemodialysis Concentrate Bicarbonate Compound Solution 31,867.53

10 Diphenhydramine HCl Expectorant (Adult) 30,077.19

11 Ezetimibe 10mg Tab 29,740.80

12 Erythropoeitin Alpha 2000 IU in 0.5ml Pre-filled Syringe (Eprex) 28,391.12

13 Calcium Lactate 300mg Tab 28,140.60

14 Fondaparinux 2.5mg/0.5ml Inj 27,370.00

15 Calcitriol 0.25mcg Cap 25,181.28

16 Amoxycillin 250mg Cap 24,942.60

17 Insulin Biphasic Isophane 100 IU/ml in 3ml Penfill (Mixtard) 24,377.97

18 Insulin Neutral (HM) 100 IU/ml in 3ml Penfill (Actrapid) 24,270.53

19 Cefuroxime Axetil 250mg Tab 24,128.00

20 Ferrous Fumarate 200mg Tab 23,683.57

TOP 20 MEDICINES PURCHASED IN HOSPITAL JASIN 2014

18

Ministry of Health (KKM) has come out with 2 essential guideline regarding High Alert Medications:- i. Guideline on Safe Use of High Alert Medications ii. Dilution Guide for High Alert Medications.

DEFINITION

Medications that bear a heightened risk of causing

significant patient harm when these medications are used in error

Eliminate medication error

Prevent adverse drug event

Ensure safe medication process

IZRUL AZWA BT MOHD LATIFF

7

No Classes / Categories Medications available in Hosp Jasin

1 Adrenergic agonists, IV Inj Adrenaline 1mg/ml Inj Noradrenaline 4mg/4ml

2 Adrenergic antagonists, IV Inj Labetalol HCl 25mg/5ml 3 Anaesthetic agents, gen-

eral, inhaled and IV

Inj Fentanyl Citrate 50 mcg/ml Inj Ketamine 10mg/ml Inj Thiopental 500mg

Inj Lignocaine HCL 2%

4 Antiarrythmias IV

Inj Amiodarone 150mg/3ml Inj Adenosine 3mg/ml Inj Lignocaine 100mg/5ml, 500mg/5ml

5 Antifibrinolytics, hemostat-ic

Inj Tranexamic acid 100mg/ml C. Tranexamic acid 250mg

6 Antithrombotic agents

Inj Streptokinase 1.5MU

Inj Enoxaparin 20mg, 40mg, 60mg

Inj Fondaparinux 2.5mg

Inj Heparin 1000 units/ml, 5000 units/ml T. Warfarin 1mg, 2mg, 3mg, 5mg

T. Dabigatran 75mg, 110mg

7 Antivenom All types of antivenom

8 Chemotherapeutic agents, parenteral and oral

Not available in Hospital Jasin

9 Dextrose, Hypertonic, 20% or greater

Inj Dextrose 5%, 10%, 20%, 50%

8 17

Drug Strength Indication Dosage

Metoclopramide Syrup

5mg/ 5ml Antiemetic; Motility agent

0.1-0.3 mg/kg TDS

(cause Extrapyramidal effects especially in children and young adults)

Metronidazole Suspension

200mg/ 5ml Antibiotic 7.5mg/kg TDS for 7days

Multivitamin Syrup 60/ 100ml Supplements Child: 2.5 ml daily

Adult: 5 ml daily

Nystatin Suspension

100,000 IU Antifungal Premature: 100,000 IU QID

Infant: 200,000 IU QID

Child & Adult: 400,000 – 600,000 IU QID

Paracetamol Syrup 120mg/ 5ml Anti-pyretic; Anti-inflammatory; Analgesic

15mg/kg TDS-QID

(max: 4gm/day)

Penicillin V

Granules (Phenoxy methylpen-icillin)

125mg/ 5ml Antibiotic 7.5-15mg/kg QID

Potassium Citrate Mist

1g/ 15ml Supplements Up to 1 year: 2.5ml TDS

1-5 years: 5ml TDS

6-12 years: 10ml TDS

Prednisolone Syrup 3mg/ 5ml Asthma 0.5-1 mg/kg OD

Promethazine Syrup 5mg/ 5ml Antihistamine/ Antiemetic

Sedative/ Hypnotic

0.2-0.5 mg/kg TDS-QID

0.5-1.5 mg/kg TDS-QID

(not recommended <2yo) Salbutamol Syrup 2mg / 5ml Bronchodilator 0.1 mg/kg QID

Sodium Bicarbonate Mixture (Paediatrics)

Heartburn, Dyspepsia

Up to 1 year: 5ml 1-5 years: 10ml in 4 to 6 divided doses

Triprolidine 1.25mg + Pseudoephedrine 30mg Syrup

Antihistamine/ Nasal decongestant

2-6 years: 2.5 ml 4-6H

7-12 years: 5 ml 4-6H

>12 years & adults: 10 ml 4-6H

PEDIATRIC SYRUP DOSING

References

Blue Book, Pharmaceutical Services Division. 2014 January. Neofax 2012. Frank Shann. Drug Doses. 16th ed. 2014; Collective P/L. Drug Formulary Melaka 2014/2015. Melaka:

16

Drug Strength Indication Dosage

Amoxicillin 200mg/ Clavulanate 28mg Suspension

228mg/ 5ml Antibiotic 10-25 mg/kg BD

Ampicillin Granules 125mg/ 5ml Antibiotic 25 mg/kg QID

Azithromycin Syrup 200mg/ 5ml Antibiotic <15kg:10mg/kg OD

15-25kg: 200mg OD

26-35kg: 300mg OD

36-45 kg:400mg OD

To be taken daily for 3 days or to be taken as a single dose on day 1, then half daily dose D2-D5

Frank Shan

15mg/kg (max:500mg) at D1, then 7.5mg/kg (max: 250mg ) D2-D5 OR

15mg/kg (max:500mg) D1-D3

Bromhexine Syrup 4mg/ 5ml Secretolytic 0.3 mg/kg TDS × 1/52

<2 yrs: 1.25 ml TDS

2-6 yrs: 2.5 ml TDS

6-12 yrs: 5 ml TDS

Bactrim Syrup

(Trimethoprim(TMP) +Sulphametho

xazole (SMX)

Each 5ml contain

TMP:40mg, SMX:200mg)

Antibiotic TMP 6mg/kg/day divided in BD Frank Shan

UTI: tmp:8-12mg/kg/day divided into BD

PCP: TMP:20mg/kg/day divide into QID

Cefuroxime Granules

125mg/ 5ml Antibiotic 10-15 mg/kg BD

Chlorpheniramine Syrup

2mg/ 5ml Anti-histamine 0.1 mg/kg TDS/QID

1-2 yrs: 1 mg BD

2-5 yrs: 1mg q4-6H

6-12 yrs: 2 mg q4-6H

(not recommended <2yo) Cloxacillin Granules 125mg/ 5ml Antibiotic 15 mg/kg QID

Erythromycin Granules

400mg/ 5ml Antibiotic 10 mg/kg QID, or 20 mg/kg BD, 15-25 mg/kg QID (severe)

Lactulose Solution 3.35g/ 5ml Laxative 0.5 ml/kg BD

PEDIATRIC SYRUP DOSING

BY: TAN XIN YIN

9

No Classes / Categories Medications available in Hosp Jasin

10 Epidural and intrathecal medications

Not available in Hospital Jasin

e.g. PCA Morphine

Epidural cocktail 11 Glyceryl Trinitrate Injection -

12 Inotropic medications, IV

Inj Digoxin 500mg/2ml Inj Dobutamine HCl 250mg/20ml Inj Dopamine HCl 40mg/ml Inj Noradrenaline 4mg/4ml

13 Insulin, subcutaneous and IV

All types of insulin

14 Magnesium Sulphate Injection

15 Neuromuscular blocking agents

Inj Atarcurium Besylate 25mg/2.5ml Inj Rocuronium Bromide 10mg/ml Inj Suxamethonium Chloride 50mg/ml Inj Vecuronium 4mg/ml

16 Opiates and Narcotics

Inj Midazolam 5mg/1ml Inj Ketamine 10mg/ml Inj Diazepam 10mg/2ml Cap. Tramadol 50mg

T. Morphine 10mg, 30mg

Syrup Morphine 10mg/10ml Syrup Methadone 5mg/ml

17 Parenteral Nutrition preparations

Not available in Hospital Jasin

18 Potassium salt injections Potassium Chloride1g/10ml 19 Sodium Chloride Solution

(greater than 0.9%) Inj Sodium Chloride 3%,

Examples of HIGH ALERT

MEDICATIONS LABELLING

High Alert Labels for Container or Product Package

High Alert Labels for Storage Shelves in Pharmacy

High Alert Labels on Ampoule or Vial

10

FLOW OF

THE OUTCOMES

DESIRED……..

≤ 6)

–

A patient can be discharged from DMTAC after fulfilling successfully any one of the following criteria: Achieve HbA1c 7% or 7.5% (Target

needs to be individualised) for at least 2 consecutive readings.

Completed a minimum of 8 visits with good medication knowledge score (100%) and MMAS > 6

Defaulted 6 months or 2 consecutive DMTAC visits, whichever is longer

Assessment of : 1. Therapeutic goal 2. Glycemic control 3. Medication adherence

4. Medication knowledge

5. Adverse reaction

Discussion of : 1. Disease progress & complications

2. Laboratory parameters

Review and discussion of self-monitoring blood glucose (Insulin dose adjustment) Identification of pharmaceutical care issues and formu-lation of a patient-specific plan that address the issues

Health advice and education Referral to other healthcare provider for interventions where appropriate

The patients will be scheduled for further appointments until glycaemic control and other laboratory parameters achieve target goals.

The initial visit of an enrolled patients will involve: Medication/ medical history

Baseline assessment of 1. Past medical/ medication

history

2. Social/ family history

3. Occupational history

4. Medication knowledge

5. Medication adherene

6. Diet & lifestyle

7. Allergy status

Education modules need to be completed before the 8th visit. The patients will be scheduled for subsequent visits. The subsequent visits shall be scheduled every 1-3 months based on patients’ need, current health status, other clinic visits and medication refill appointments.

15

BY: LOW JIA HUI

14

WHAT IS DIABETES MTAC?

An ambulatory care service offered by pharmacists in

collaboration with the physicians to help patients achieve

better adherence level and glycemic control.

Patients enrolled will be follow-up for a minimum of 8 visits

where they will receive the following services by pharmacists:

Medication adherence assessment

Identification & management of drug-related

problems

Medication counselling

Clinical outcomes monitoring

How it works?

A patient will be selected based on the following criteria:

A current patient at the hospital/ clinic where the DMTAC is carried out

Patients with uncontrolled diabetes despite optimal medications

Patient non-compliant to medication (Morisky Medication Adherence Scale, MMAS ≤ 6)

Patient with HbA1C > 8%

Patient with co-morbidities/ multiple medications

Patient with macro- & micro– vascular complications

After a patient is selected, the patient needs to be advised on :

DMTAC mission

Anticipated benefits to the patients or care givers

Goals for patients

Patients rights and responsibility in the program

Upon agreeing to be enrolled, the patient will sign an informed consent form that allows their

information to be released or shared with other health care providers involved in their care for providing

critical information needed for coordination of their care.

OBJECTIVES

Improve patients’ knowledge

towards medication and disease

Increase patients’ adherence

Reduce adverse effects and

complications

Educate patients about diabetes

complications, proper self-

management, use of medications

and self-care devices

Assist physicians in monitoring

patient’s drug therapy and medical conditions

DRUG COMPARISON BETWEEN HEPARIN, ENOXAPARIN AND

FONDAPARINUX

Heparin Enoxaparin Fondaparinux

Indica-tion

i) Prophylaxis and treat-ment of venous throm-bosis and Pulmonary Embolism

ii) Treatment of myocardial infarction and arterial embolism

iii) Prevention of clotting in arterial and heart surgery and for preven-tion of cerebral throm-bosis

i) Prevention of Deep Vein Thrombosis (DVT) especially in perioperative and high risk surgical cases

ii) Treatment of DVT & PE

iii) Unstable angina and non Q wave Myocardial Infarction

i) Treatment of acute Deep Vein Thrombosis & Pulmonary Embolism(PE) ii) Prevention of venous thromboembolic events (VTE) in orthopedic surgery

iii) Treatment of unstable angina or non ST-segment elevation myocardial infarction (UA/NSTEMI) in patients for whom urgent invasive management (PCI) is not indicated

iv) Treatment of ST segment elevation myocardial infarction (STEMI) in patients managed with thrombolytics or are not receiving other forms of reperfusion

Pregnan-cy Risk Factor

C B B

Ng Shy Pyng

11

Heparin Enoxaparin Fondaparinux

Dose i) By IV injection, loadig dose of 5000 units (10000units in severe pulmonary embolism) followed by continuous infusion of 15-25 units/kg/hr. By SC injection (for DVT) of 15000units every 12hours. Small adult or child, lower loading dose then, 15-25units/kg/hr by IV infusion, or 250 units/kg every 12 hours by SC injection

ii) As 1) for unstable angina and acute peripheral arterial occlusion

iii) Prophylaxis in general surgery, by SC injection, 5000 units 2 hour before surgery then every 8-12 hours for 7 days or until patient is ambulant, during pregnancy 5000-

10000 units every 12 hours. An adjusted dose regime may be used for major orthopaedic surgery or low molecular weight heparin may be selected

i) Prophylaxis for DVT especially in surgical patients: moderate risk, 20mg SC approximately 2hours before surgery then 20mg every 24hours for minimum 7-10 days, high risk (e.g. orthopaedic surgery, medical patients, 40mg every 24 hours for at least 6 days until patient ambulant max-imum 14days) ii) 1.5mg/kg every 24 hours, usually for 5days and until adequate oral anticoagulation established. iii) 1mg/kg every 12 hours, usually 2-

8days

i) BW < 50kg: 5mg once daily, BW 50-100kg:7.5mg once daily, BW>100kg : 10mg once daily . Treatment for at least 5days and until adequate oral anticoagulation is estab-lished (INR 2-3) . Concomi-tant treatment with vitamin K antagonists should be initiated within 72 hours, usual duration 5-9days. ii) 2.5mg once daily given by SC, administered 6 hour following surgical closure provided hemostasis has been established. Usu-al duration 5-9days; for hip fracture patients, an extend-ed course up to 24 days

iii))Adult more than 18 years: 2.5mg once daily given by SC up to 8days or until hospital discharge. If patients needs to undergo PCI, unfractionated heparin to be administered as per local practice protocol, taking into account the patient’s bleeding risk and time of last dose of fondaparinux. Fondaparinux may be restarted no earlier than 2 hours after sheath removal iv) Adult more than 18 year: 2.5mg once daily, first dose to be given IV, subsequently dose to be given SC up to a max of 8days or until hospital discharge. If patients need to undergo nonprimary PCI, unfractionated heparin to be administered as per local practice protocol, taking into account the patient’s bleeding risk and time of last dose of fondaparinux. Fondaparinux may be re-started no earlier than 3 hour after sheath removal

12

Heparin Enoxaparin Fondaparinux

Cost 1000iu=RM13.60/vial 5000iu=RM16.60/vial

20mg=RM18.90/syringe

40mg=RM25.40/syringe

60mg=RM31.10/syringe

RM 25.40/syringe

Mecha-nism of action

Potentiates the action of antithrombin III and thereby inactivates thrombin( as well as activated coagulation factors IX, X, XI, XII and plasmin) and prevents the conversion of fibrinogen to fibrin; heparin also stimulates release of lipoprotein lipase( lipoprotein lipase hydrolyzes triglycerides to glycerol and free fatty acids)

Derived from porcine heparin that undergoes benzylation followed by alkaline depolymerization. Enoxaprin has a higher ration of antifactor Xa to antifactor IIa activity than unfractioned heparin

A synthetic pentasaccharide that cause an antithombin III-mediated selective inhibition of factor Xa. Neutralization of factor Xa interrupts the blood coagulation cascade and inhibits thrombin formation and throm-bus development

Pharmaco-dynamics/

kinetics

Onset: Anticoagulation: Immediate (IV); approx 20-30 min (SC).

Absorption: Absorbed from systemic circula-tion.

Distribution: Plasma protein binding: Exten-sive.

Metabolism: Partially metabolised in the liver to uroheparin (partially desulfated heparin); appears to be removed from the circulation mainly by the reticuloendothelial system and may localise on arterial venous endothelium.

Excretion: Via urine (as metabolites, or up to 50% as unchanged drug after admin of large doses). Half-life: 1-6 hr.

Onset: 3-5 hr.

Absorption: Rapidly and almost completely absorbed. Bioavailabil-ity: Approx 100%. Peak plasma concentrations: 1-5 hr.

Distribution: Volume of distribution: 4.3 L. Plas-ma protein binding: Does not bind to heparin binding proteins.

Metabolism: Hepatically metabolised.

Excretion: Via urine (40% as unchanged drug; 10% as active metabolites). Elimination half-life: Approx 4-5 hr.

Onset: Time to peak: 2-3hours

Absorption: Rapid and complete

Bioavailability: 100%

Distribution: Volume of distribution:mainly in blood. Plasma protein binding ≥94% to antithrombin III

Excretion: Urine (77% unchanged drug)

References

Drug Information Handbook 2012-2013: A Comprehensive Resource for all Clinicians and Healthcare Professionals.Lexicomp

Ministry Of Health Medicines Formulary 2014

MIMS Malaysia

13