16.7 Changing from One Opioid Agonist to Another

See also Frequently Asked Questions About Heroin, Morphine, and the Opiates - Heroin/Morphine FAQ

There is a considerable tolerance present when middle to high doses of one opioid agonist are consumed before changing from one agonist to another. Changes are in this case not risky.

The change from pure opioid agonists to agonists/antagonists and to partial agonists always causes a more or less distinct withdrawal syndrome. The change in the opposite direction is on the other hand, possible without complaints.

The change from an opioid with a short half-life to an opioid with a longer half-life, due to different kinetics and cumulations, can lead to considerable under dosing in the first few days (see Abb.29 & 30).

By changing from one opioid to another or by distributing the daily dose over several combined administered opioids, the calculation base is always the measured day-before opioid dose in MDQ.

When consuming opioids twice a day, the daily dose is then (usually evenly) distributed over two doses and possible increases in dose that are possible from day to day are considered as well.

A maximum single dose is calculated out of the calculated total daily dose, when short-lasting opioids are consumed more than twice a day. In this case, one has a maximum possible daily dose worked out from the number of consumed single-doses (through prescription defined or left open).

 

15.7.1 Changing from Methadone to Short-Lasting Opioids

Changing from peroral or injected methadone to short-lasting opioid agonists such as injected heroin, DAM-cigarettes and morphine is kinetically unproblematic.

The methadone consumed the day before is taken as the reference value. If the last methadone dose was consumed yesterday, the dose from the previous day in MDQ is converted (Methadone in mg = Methadone in MDQ, as the MDQ-Factor = 1) thus giving the daily dose of the new opioid. This daily dose of the new opioid needs to be converted from the unit MDQ into mg.

If no methadone has been consumed for a day or more, the dose needs to be linearly reduced by 20% per absent day due to the loss of tolerance (see chapter 16.4).

Example. 13: Changing from 100 mg Methadone to 3 i.v. Heroin-inj./day

 

Me p.o.

He i.v.

MDQ

Calculation

Methadone-Dose of previous day

100 mg

 

100

100 MDQ *3/2= 150 mg Heroin

1 th day of change

0

3*150 mg

150

 
2 th day of change

0

3*225 mg

225

 

MDQ-Factor of Heroin is 3: (Methadone in mg) * 3 = (Heroin in mg). Therefore the first single dose is: (Heroindosis in mg) = ((Methadon in mg)* 3/2). While changing the first-day-dose was risen 50% as allowed.

 

When changing from methadone to more than 2 heroin injections a day, half of the methadone dose, in MDQ, consumed on the day before can be injected as a single dose of heroin (examples 13 & 15).

Example. 14: Changing from 100 mg Methadone to 2 i.v. Heroin-inj./day

 

Me p.o.

He i.v.

MDQ

Calculation

Methadone-Dose of previous day

100 mg

 

100

100 MTQ *3/2= 150 mg Heroin

1 th day of change

0

2*150 mg

100

150 mg * 1.5

2 th day of change

0

2*225 mg

150

 

While changing to two daily doses of heroin, the first-day-dose (measured in MDQ) could not be risen.

 

Changing from methadone to two heroin injections a day follows analogue: the daily dose is simply distributed over 2 injections a day (example 14).

Example 15: Changing from 50 mg methadone to heroin i.v. (3 inj./day)

 

Me p.o.

He i.v.

MDQ

Calculation

Methadone-Dose of previous day

50

 

50

50/2 = 25 MTQ
= 75 mg Heroin

1 th day of change

0

3*75 mg

75

3*(75/2)@ 110 mg

2 th day of change

0

3*110 mg

110

 

 

The contradictions in our equivalence table become clearly obvious when changing from methadone to heroin i.v.. The flash effect of injected heroin only starts to decrease at daily doses of 600 mg(see picture .27). When changing, the withdrawal-preventing effect of heroin is replaced, the flash-effect stays

Example. 16: Changing from methadone to methadone + 2 heroin injections

 

Me p.o.

He i.v.

MDQ

Calculation

Methadone-Dose of previous day

50 mg

 

50

50*1.5 = 75 MTQ

= 25mg Me + 150mg He

1th day of change

25 mg

2*75mg

75

75*1.5 = 112.5 MTQ

@ 25mg Me + 260 mg He

2 th day of change

25 mg

2*130mg

111.7

 

 

On the other hand, intravenous injected heroin reaches the tolerance dose thus also the maximum effect in relation to analgesia and persistent euphoria (withdrawal-preventing opioid saturation) already at 300 mg/day(see picture 27). When changing from methadone to heroin i.v., the withdrawal-preventing opioid saturation as maximum-effect dose (tolerance dose), becomes more relevant. Our thoughts let us think that a MDQ-Factor of 3 for heroin i.v. seems sensible. In example 16, one is changing from methadone alone to a combination of methadone and 2 daily injections.

Example. 17: Changing from 100 mg Methadone to Morphine ret. Tabs.

 

Methadone

Morphine ret.

MDQ

Calculation

Methadone-Dose of previous day

100 mg

 

100

6*100/2=300mg

1th day of change

0

2*300 mg

100

 
2 th day of change

0

2*300 mg

100

 

 

The change from methadone to morphinepentasulphate in retard form is shown in example 17. The daily dose is not increased when doing this change.

Example. 18: Changing from 60 mg methadone to DAM-cigarettes

 

Methadone

mg

DAM-cigarettes

Methadone-Dose of previous day

60

--

1th day of change

45

6 Stück

2 th day of change

30

9 Stück

3 th day of change

20

12 Stück

4 th day of change

15

15 Stück

5 th day of change

10

18 Stück

6 th day of change

5

21 Stück

7 th day of change

0

21 Stück

 

The change from methadone to DAM-cigarettes is not problematic when methadone has been consumed in small doses previously. As long as the methadone dose has remained under 50 mg, there can be an abrupt change without any transition. When doses of methadone of 50 mg or more have been consumed it is recommended that along with the DAM-cigarette full-dosing, that a parallel decreasing methadone dose is prescribed (pushing out methadone). Methadone has such a strong effect over 30mg that when taken in parallel, the effects of the DAM-cigarettes stay covered.

15.7.2 Changing from injecting Heroin to Methadone

Fig.29: Course of the Withdrawal-inhibiting Opioid Saturation when Changing from Heroin to Methadone. Without any previous intake of methadone the withdrawal-preventing opioid saturation crashes unpleasantly down in the first days where methadone is consumed alone.

 

When, for example, for holiday take-away doses, there has to be a change from short-lasting opioids with little cumulation (heroin, DAM-cigarettes, mo i.v. and morphinepentasulphate) to methadone with the longer half-life value, the result is only a slight effect in the first few days, without any previous cumulation. After changing from heroin to methadone the steady-state thus sufficient withdrawal-preventing opioid saturation is only reached after a few days.

Fig.30: Course of Withdrawal-inhibiting Opioid Saturation when Changing from Heroin to Methadone.
Better: To begin previous to holidays, with methadone
® the withdrawal-inhibiting opioid saturation does not crash down

 

Either the missing previous methadone cumulation is compensated for by prescribing a 50% higher dose for the first two days holiday or (see variance 1 in example.19/20/21) or the methadone is consumed additionally already a few days before going on holiday (see Abb.30 and Var 2 in example.19/20/21).

Example. 19: Changing from Heroin i.v. (daily dose 400 mg / day) to Methadone p.o. and back (holidays)

 

last two days before holidays

1th holiday

2th holiday

other holiday

back from holidays

Heroin

> 400 mg /Tag

0

0

0

> 400 mg /Tag

Methadone Var. 1

0 mg

150 mg

120 mg

100 mg

0

Methadone Var. 2

100

100 mg

100 mg

100 mg

0 bis 100 mg

 

Example. 20: Changing from Heroin i.v. 300 mg / day to Methadone p.o. and back (holidays)

 

last two days before holidays

1th holiday

2th holiday

other holiday

back from holidays

Heroin

300 mg / Tag

0

0

0

300 mg / Tag

Methadone Var. 1

0

100 mg

75 mg

75 mg

0

Methadone Var. 2

75 mg

75 mg

75 mg

75 mg

0

 

Example. 21: Changing from Heroin i.v. 90 mg / day to Methadone p.o. and back (holidays)

 

last two days before holidays

1th holiday

2th holiday

other holiday

back from holidays

Heroin

90 mg / Tag

0

0

0

90 mg / Tag

Methadone Var. 1

0

30

30

30

0

Methadone Var. 2

30

30

30

30

0

 

Giving more than 100 to 120 mg methadone per day is hardly justifiable except for this change, and can be problematic due to the increased possibilities to abuse the high dose.

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