I have been considering the idea of throwing a couple of hundred...

I have been considering the idea of throwing a couple of hundred bucks behind the moxduo tablet, but have some reservations of backing a new product that seems not to have retained usual orally delivery issues as outlined below that can be addressed by a different route of delivery.
I was hoping that there would be some learned QRX holders who could enlighten me.
Thanks in advance.

Oral vs transdermal delivery.

GI tract bypassed transdermally

Tablets generally require higher dose of opiod to ensure that after 1st pass metabolism, a therapeutic blood concentration is achieved.
Passing through the GI system creates a series of side effects including constipation, headaches and dizziness.

Steady state of drug administration.

A tablet provides an initial bolus dose of opiod, following which the opiod begins clearance from the system, until blood concentration levels become un-therapeutic, at about the 6-8hr point.
A transdermal patch blood concentration level rises gradually to the therapeutic level and is maintained at this point for 3 days.

Bolus dose not required.

Administration of an opiod requires a blood concentration level of about 8ng/ml to be therapeutic.
For a tablet to have effect over 6hrs it requires an initial dose of 20-30ng/ml, before clearance occurs. This rapid absorption of high levels can produce a euphoric state.
A transdermal patch will gradually rise to a chosen level, for example 10-12ng/ml and sustain it there. This mechanism also allows the level of concentration to be chosen, and avoids the high levels that tablets provides.

No break through pain.

As clearance occurs from tablet administration, the sudden drop from therapeutic to un-therapeutic levels creates breakthrough pain, which means every 6-8 hours pain returns at quite high intensities. If the drug concentration levels drop too low before the required duration patients will end up taking tablets more frequently than required and at higher doses or quantities to maintain the controlled pain state.
The problem is empathized at nighttime, when breakthrough pain will effect sleep, compounding the issues of chronic pain.
A transdermal patch will eliminate breakthrough pain by sustaining the blood concentration level.

Delayed onset of tolerance.
As described, a tablet requires a bolus dose to maintain its effect over 6-8hrs.
Unfortunately the body adapts to levels of opiod and requires increased dose over time to achieve the same effect. The higher the dose the in the blood the quicker the body adapts to the lower dose, meaning a more rapid escalation in dosage required.
The lower blood concentrations needed with a transdermal patch means tolerance is significantly delayed.

Eliminate euphoria and potential drug abuse.

Euphoria is achieved by high levels of opiods. This is easily achieved by oral administration of tablets. Blood concentration levels rise in a linear fashion when taken orally until euphoria is achieved. The risk of overdose is created particularly when tolerance means higher levels are needed to achieve euphoria.
The state of euphoria is a risk in leading to drug abuse.

A transdermal patch does not allow euphoria.
Amazingly skin acts as a protective barrier and works under what’s called “sink conditions” which means once a certain level of opiod is administered, a saturation point is reached and no more enters the systemic system. This saturation point is below euphoric levels. You can put 10 patches on and euphoria can not be achieved, nor overdose.

Abuse and tampering.

Tablets can be easily tampered with to collect the opiod concentrate to be abused as an injected drug. The patch is designed to make tampering if not impossible, close to it.

Compliance and convenience
Certain population groups including the elderly find it difficult to swallow tablets.
The easy application of a patch provides an alternative and the convenience of applying a patch once every 3 days compared to taking tablets on 9 occasions over the same time period is self evident.


Would love to hear some objective opinions.